EGFR

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1023	Erlotinib HCl (OSI-744)	<1 mg/mL	4 mg/mL	<1 mg/mL
S1025	Gefitinib (ZD1839)	<1 mg/mL	89 mg/mL	4 mg/mL
S1028	Lapatinib (GW-572016) Ditosylate	<1 mg/mL	100 mg/mL	<1 mg/mL
S1011	Afatinib (BIBW2992)	<1 mg/mL	97 mg/mL	15 mg/mL
S1006	Saracatinib (AZD0530)	<1 mg/mL	35 mg/mL	31 mg/mL
S9786	BDTX-189	<1 mg/mL	100 mg/mL	''''<1 mg/mL
S6899	Licochalcone D	-1 mg/mL	100 mg/mL	-1 mg/mL
S6897	Epertinib hydrochloride	<1 mg/mL	100 mg/mL	<1 mg/mL
S8584	Theliatinib (HMPL-309)	-1 mg/mL	47 mg/mL	'-1 mg/mL
S6868	Alflutinib (AST2818) mesylate	<1 mg/mL	20 mg/mL	<1 mg/mL
S8920	(Rac)-JBJ-04-125-02	<1 mg/mL	100 mg/mL	'''<1 mg/mL
S8852	Pyrotinib (SHR-1258) dimaleate	<1 mg/mL	<1 mg/mL	''<1 mg/mL
S6805	Tyrphostin AG-528	˂1 mg/mL	61 mg/mL	5 mg/mL
S1046	Vandetanib (ZD6474)	<1 mg/mL	4 mg/mL	<1 mg/mL
S2150	Neratinib (HKI-272)	<1 mg/mL	5 mg/mL	<1 mg/mL
S1019	Canertinib (CI-1033)	<1 mg/mL	2 mg/mL	9 mg/mL
S2111	Lapatinib (GW-572016)	<1 mg/mL	100 mg/mL	''<1 mg/mL
S1143	AG-490 (Tyrphostin B42)	<1 mg/mL	58 mg/mL	'6 mg/mL
S1167	CP-724714	<1 mg/mL	94 mg/mL	94 mg/mL
S2727	Dacomitinib (PF-00299804)	<1 mg/mL	19 mg/mL	<1 mg/mL
S1173	WZ4002	<1 mg/mL	13 mg/mL	<1 mg/mL
S2192	Sapitinib (AZD8931)	<1 mg/mL	40 mg/mL	<1 mg/mL
S1194	CUDC-101	<1 mg/mL	20 mg/mL	<1 mg/mL
S2728	AG-1478 (Tyrphostin AG-1478)	<1 mg/mL	25 mg/mL	13 mg/mL
S1079	PD153035 HCl	<1 mg/mL	0.5 mg/mL	<1 mg/mL
S1392	Pelitinib (EKB-569)	<1 mg/mL	13 mg/mL	<1 mg/mL
S1056	AC480 (BMS-599626)	<1 mg/mL	113 mg/mL	20 mg/mL
S1486	AEE788 (NVP-AEE788)	<1 mg/mL	88 mg/mL	<1 mg/mL
S7000	AP26113-analog (ALK-IN-1)	<1 mg/mL	45 mg/mL	106 mg/mL
S2205	OSI-420	<1 mg/mL	83 mg/mL	<1 mg/mL
S1170	WZ3146	<1 mg/mL	93 mg/mL	<1 mg/mL
S2752	HER2-Inhibitor-1	<1 mg/mL	100 mg/mL	3 mg/mL
S1179	WZ8040	<1 mg/mL	96 mg/mL	3 mg/mL
S2185	Allitinib (AST-1306)	<1 mg/mL	124 mg/mL	<1 mg/mL
S7284	Rociletinib (CO-1686)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1342	Genistein (NPI 031L)	<1 mg/mL	54 mg/mL	''2 mg/mL
S2755	Varlitinib	<1 mg/mL	6 mg/mL	<1 mg/mL
S2922	Icotinib (BPI-2009H)	<1 mg/mL	78 mg/mL	'7 mg/mL
S2784	TAK-285	<1 mg/mL	110 mg/mL	54 mg/mL
S2867	WHI-P154	<1 mg/mL	75 mg/mL	<1 mg/mL
S2554	Daphnetin	<1 mg/mL	35 mg/mL	<1 mg/mL
S7039	PD168393	<1 mg/mL	73 mg/mL	<1 mg/mL
S2895	Tyrphostin 9	<1 mg/mL	56 mg/mL	56 mg/mL
S7206	CNX-2006	<1 mg/mL	100 mg/mL	29 mg/mL
S8009	AG-18	<1 mg/mL	37 mg/mL	37 mg/mL
S0711	Canertinib dihydrochloride	20 mg/mL	100 mg/mL	'''<1 mg/mL
S6525	AG 555	<1 mg/mL	64 mg/mL	'64 mg/mL
S7298	AZ5104	<1 mg/mL	97 mg/mL	23 mg/mL
S8724	Lazertinib	<1 mg/mL	4 mg/mL	<1 mg/mL
S7297	Osimertinib (AZD9291)	<1 mg/mL	99 mg/mL	'43 mg/mL
S7557	CL-387785 (EKI-785)	<1 mg/mL	63 mg/mL	'<1 mg/mL
S6509	AG 494	<1 mg/mL	56 mg/mL	4 mg/mL
S8362	Tucatinib (Irbinitinib, ONT-380)	<1 mg/mL	96 mg/mL	15 mg/mL
S8294	Olmutinib (BI 1482694)	<1 mg/mL	97 mg/mL	23 mg/mL
S6523	RG14620	<1 mg/mL	55 mg/mL	'6 mg/mL
S6546	PD153035	<1 mg/mL	6 mg/mL	<1 mg/mL
S6541	MTX-211	<1 mg/mL	24 mg/mL	<1 mg/mL
S6813	Mobocertinib (TAK788)	<1 mg/mL	9 mg/mL	<1 mg/mL
S2250	(-)-Epigallocatechin Gallate	23 mg/mL	72 mg/mL	83 mg/mL
S7786	Erlotinib (OSI-774)	<1 mg/mL	78 mg/mL	''''15 mg/mL
S0070	Gefitinib-based PROTAC 3	<1 mg/mL	100 mg/mL	100 mg/mL
S5098	Gefitinib hydrochloride	1 mg/mL	8 mg/mL	1 mg/mL
S7810	Afatinib (BIBW2992) Dimaleate	<1 mg/mL	100 mg/mL	<1 mg/mL
S7971	AZD3759	<1 mg/mL	91 mg/mL	20 mg/mL
S7358	Poziotinib (HM781-36B)	<1 mg/mL	98 mg/mL	<1 mg/mL
S8229	Brigatinib (AP26113)	<1 mg/mL	1 mg/mL	43 mg/mL
S5078	Osimertinib mesylate	-1 mg/mL	9 mg/mL	-1 mg/mL
S6698	TQB3804 (EGFR-IN-7)	<1 mg/mL	<1 mg/mL	<1 mg/mL
S0360	EGFR Inhibitor	˂1 mg/mL	83 mg/mL	2 mg/mL
S8412	Naquotinib(ASP8273)	<1 mg/mL	52 mg/mL	100 mg/mL
S2406	Chrysophanic Acid	<1 mg/mL	5 mg/mL	<1 mg/mL
S7824	Nazartinib (EGF816)	<1 mg/mL	99 mg/mL	99 mg/mL
S3759	Norcantharidin	-1 mg/mL	33 mg/mL	-1 mg/mL
S1054	AG99	<1 mg/mL	41 mg/mL	'<1 mg/mL
S0151	AG-1557	<1 mg/mL	40 mg/mL	3 mg/mL
S2115	RG 13022	<1 mg/mL	53 mg/mL	'5 mg/mL
S7926	Lifirafenib (BGB-283)	<1 mg/mL	95 mg/mL	''95 mg/mL
S4667	Lidocaine hydrochloride	54 mg/mL	54 mg/mL	'54 mg/mL
S8036	Butein	<1 mg/mL	55 mg/mL	55 mg/mL
S8242	EAI045	<1 mg/mL	76 mg/mL	<1 mg/mL
S8814	TAS6417	<1 mg/mL	79 mg/mL	'79 mg/mL
S9414	Cyasterone	-1 mg/mL	100 mg/mL	-1 mg/mL
S6809	SU5214	<1 mg/mL	50 mg/mL	<1 mg/mL
S8817	Almonertinib (HS-10296)	<1 mg/mL	100 mg/mL	'6 mg/mL
S8741	Avitinib (AC0010)	<1 mg/mL	97 mg/mL	97 mg/mL
S8312	NSC228155	<1 mg/mL	15 mg/mL	<1 mg/mL
S6530	EBE-A22	<1 mg/mL	9 mg/mL	<1 mg/mL

亜型選択性的な製品

EGFR製品

All (88) EGFR阻害剤(85) EGFR抗体(1) EGFR活性剤(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1023	Erlotinib HCl (OSI-744) Erlotinib HCl (OSI-744, CP358774, NSC 718781) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.	Nat Cell Biol, 2021, 23(4):377-390 Sci Adv, 2021, 7(10)eabe8671 Proc Natl Acad Sci U S A, 2021, 118(19)e2019580118	Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone.
S1025	Gefitinib (ZD1839) Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.	Nat Cell Biol, 2021, 23(4):377-390 Theranostics, 2021, 11(2):824-840 Theranostics, 2021, 11(6):2594-2611	Perturbation of EGFR by its ligand EGF and gefitinib (ZD-1839 Iressat; inhibits EGFR) produces opposite responses in the predicted EGFR target genes SOCS2 and NR2E1.
S1028	Lapatinib (GW-572016) Ditosylate Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.	Nat Cell Biol, 2021, 23(4):377-390 J Transl Med, 2021, 19(1):184 Cancer Med, 2021, 10(7):2370-2379	Combination of NVP-AEW541 and lapatinib cooperatively inhibits the growth of NVP-AEW541 resistant murine rhabdomyosarcoma primary cell cultures with Igf1r/Her2 complexes. Cell viability assay for Naïve, untreated (U20325; A) and NVP-AEW541 innately resistant mouse rhabdomyosarcoma primary culture (U44676; B) treated with varying concentrations of NVP-AEW541, lapatinib, or a combination of both. Naïve cells (U20325) were sensitive to NVP-AEW541, but lapatinib had no cooperativity. In contrast, NVP-AEW541 at moderate doses increased cell growth in resistant cell cultures (U44676). However, this paradoxical effect was reduced by the addition of lapatinib, although lapatinib treatment alone had very little effect. C, the NVP-AEW541 resistant primary tumor cell line (U44676) was treated with DMSO, 5 μmol/L lapatinib, 5 μmol/L NVP-AEW541, and a combination of 5 μmol/L NVP-AEW541+lapatinib for 25 minutes and Western blot analysis was done on lysates for p-Igf1r and p-Her2.
S1011	Afatinib (BIBW2992) Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.	Cancer Cell, 2021, S1535-6108(20)30609-7 Nat Cell Biol, 2021, 23(4):377-390 Cancer Res, 2021, canres.2276.2020	Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay.
S1006	Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.	Int J Cancer, 2021, 10.1002/ijc.33606 Oncogene, 2021, 40(14):2567-2580 FASEB J, 2021, 35(5):e21598	C and D, in vivo subcutaneous tumor growth curves (C) and tumor weight quantification of intersected subcutaneous tumor tissues (D) of Huh7 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n =18). , P < 0.05. E and F,in vivo subcutaneous tumor growth curves (E) and tumor weight quantification of intersected subcutaneous tumor tissues (F) of SK-Hep1 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n = 18). , P < 0.05.
S9786^新	BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
S6899^新	Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and MET activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S6897^新	Epertinib hydrochloride Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.
S8584^新	Theliatinib (HMPL-309) Theliatinib (HMPL-309) is a highly potent EGFR inhibitor with Ki value of 0.05 nM against the wild type EGFR and IC50 values of 3 nM and 22 nM against EGFR and EGFR T790M/L858R mutant. It demonstrats 50 fold greater selectivity for EGFR compared to 72 other kinases.
S6868^新	Alflutinib (AST2818) mesylate Alflutinib (AST2818) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.
S8920^新	(Rac)-JBJ-04-125-02 JBJ-04-125-02 is a mutant-selective allosteric inhibitor of EGFR.
S8852^新	Pyrotinib (SHR-1258) dimaleate Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.	Clin Transl Med, 2020, 10(8):e254
S6805^新	Tyrphostin AG-528 Tyrphostin AG-528 (Tyrphostin B66) is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity.
S1046	Vandetanib (ZD6474) Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).	J Clin Endocrinol Metab, 2021, dgab020 Drug Metab Dispos, 2021, 49(1):53-61 J Enzyme Inhib Med Chem, 2021, 36(1):163-174	Vandetanib reduced extracellular nitrite levels in endothelial cells. MS1 endothelial cells (ECs) were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]), 50 ng/mL of vascular endothelial growth factor (VEGF) or matched vehicle (PBS; 0.5 hours), and L-arginine and soluble N-ethylmaleamide sensitive factor attachment protein (SNAP) added (1.5 hours). Vandetanib lowered nitrite levels in MS1 Ecs (P0.0003). VEGF was used a positive control and increased nitrite levels (*P0.02). These findings indicate that vandetanib lowered endothelial cell NO levels.
S2150	Neratinib (HKI-272) Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.	Cancer Med, 2021, 10(7):2370-2379 Cancer Cell, 2020, 37(2):183-199 Acta Neuropathol, 2020, 17	HER2 mutations V777L, D769H, V842I, G309A induce gain-of-function over HER2 WT in MCF10A mammary epithelial cells. B, HER2 WT, L755S, and del.755–759 cells were grown in Matrigel in the presence of DMSO vehicle (0.5%), neratinib (0.5 μmol/L) or gefitinib (0.5 μmol/L). Phase contrast images were obtained as in A. C, MCF10A-HER2 WT or mutants were seeded in soft agar. After 7 days of growth, they were treated with DMSO vehicle (0.5%), lapatinib (0.5 μmol/L) or neratinib (0.5 μmol/L) for an additional week. Error bars represent 95% highest posterior density intervals. *, Significant difference between the HER2 mutant and HER2 WT; #, the effect of inhibitor treatment was significant (95% highest posterior density interval did not contain 0 for both). D, photomicrographs of the colonies in soft agar on day 12, magnification ×40.
S1019	Canertinib (CI-1033) Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3.	Acta Physiol (Oxf), 2021, 10.1111/apha.13661 ACS Chem Biol, 2021, 10.1021/acschembio.0c01000 Genome Med, 2020, 18;12(1):17	(B–C) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 lg). The cells were then treated with Erlotinib (20 lM), Gefitinib (20 lM), Lapatinib (20 lM), CI-1033 (8 lM), LY294002 (20 lM) and Bortezomib (20 lM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (±SD) of duplicate values of a representative experiment that was independently repeated for five times.
S2111	Lapatinib (GW-572016) Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.	Nat Cell Biol, 2021, 23(4):377-390 Mol Cell, 2021, 81(4):708-723.e5 Cell Rep, 2021, 34(10):108822	Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using speciﬁc antibodies.
S1143	AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42, Zinc02557947) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.	Front Nutr, 2021, 8:649640 Oncol Rep, 2021, 10.3892/or.2021.7926 Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7	IL6 normally induces WASF3 expression in MDA231 cells, but co-treatments with AG490 (a pan-JAK inhibitor) show a dose-dependent reduction of both WASF3 levels and activated STAT3 levels.
S1167	CP-724714 CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.	Int J Mol Sci, 2020, 22(1)E82 NPJ Breast Cancer, 2020, 6:30 Cancers (Basel), 2019, 11(3)
S2727	Dacomitinib (PF-00299804) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2.	Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w Nat Commun, 2020, 11(1):4607 Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2321
S1173	WZ4002 WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM in BaF3 cell line; does not inhibit ERBB2 phosphorylation (T798I).	Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w Cell Res, 2020, 10.1038/s41422-020-00409-1 Cancer Res, 2020, 80(21):4655-4667	Antitum o r activity of WZ4002 and/or E7050 in mouse xenograft models of human tumors. SCID mice-bearing PC-9/Vec (A), PC-9/HGF#5 (B), H1975 (C), or HCC827ER (D) tumors were administered 25 mg/kg WZ4002 and/or E7050 once daily for 14 to 21 days. Tumor volume was measured using calipers on the indicated days. Mean?SE tumor volumes are shown for groups of 4 to 5 mice.
S2192	Sapitinib (AZD8931) Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.	Nature, 2020, 584(7822):608-613 Nature, 2020, 584(7822):608-613 J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X
S1194	CUDC-101 CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.	Cancer Sci, 2020, 112(1):133-143 Anticancer Drugs, 2020, 31(2):158-168 NPJ Breast Cancer, 2020, 6:30	(a) Decay-corrected microPET/CT scan of MDA-MB-231 tumor bearing mice (n = 4) at 2, 4, and 24 h after i.v. injection of [64Cu]7. The image obtained with coinjection of CUDC-101 (20 mg/kg body weight) is shown for a 24 h blockade. Tumors are indicated by arrows. (b) Decay-corrected region-of interest (ROI) analysis on microPET images of the tumor uptake of [64Cu]7 with or without coinjection of CUDC-101 (20 mg/kg body weight). , P < 0.05; *, P < 0.01.
S2728	AG-1478 (Tyrphostin AG-1478) AG-1478 (Tyrphostin AG-1478, NSC 693255) is a selective EGFR inhibitor with IC50 of 3 nM in cell-free assays, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR. AG-1478 (Tyrphostin AG-1478) inhibits encephalomyocarditis virus (EMCV) and hepatitis c virus (HCV) by targeting phosphatidylinositol 4-kinase IIIα (PI4KA).	Theranostics, 2021, 11(3):996-1015 Oncogenesis, 2021, 10(3):25 Am J Transl Res, 2021, 13(2):708-718	A549 cells were treated with G15 (a specific antagonist of GPR30, 1 uM), AG1478 (a potent antagonist of EGFR, 10 uM), BPA (10^-5 M) alone for 15 min or BPA after a 90-min pretreatment with G15 or AG1478 for 15 min. Then the expression of p-ERK1/2 and total ERK1/2 were measured by western blot analysis.
S1079	PD153035 HCl PD153035 HCl (SU-5271 HCl, AG1517 HCl, ZM 252868 HCl) is a potent and specific inhibitor of EGFR with K_i and IC50 of 5.2 pM and 29 pM in cell-free assays; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.	Int J Mol Sci, 2021, 22(8)3945 FEBS Lett, 2021, 595(5):563-576 FEBS Lett, 2021, 10.1002/1873-3468.14032	IGF-1 and IL-1β mediated induction of Bcl-2 expression involves EGFR. (A) Bcl-2 mRNA levels in AALEBs treated with IGF-1 or IL-1β in the presence or absence of two EGFR tyrosine kinase inhibitors, EKB-569 (1 μM) or PD153035 (1 μM).
S1392	Pelitinib (EKB-569) Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Pelitinib (EKB-569) also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282 nM, 800 nM and 1255 nM, respectively. Phase2.	Mol Cancer Ther, 2020, 5;molcanther.1131.2019 Nat Cell Biol, 2019, 21(6):778-790 Korean J Parasitol, 2017, 55(5):491-503	HBMEC were preincubated with the indicated concentrations of either ErB1/2/4 inhibitor (Pelitinib; EKB-569), and cells were then infected for 4 h with the unencapsulated strain, MC58 siaD. The numbers of adherent (black bars) and invasive (gray bars) bacteria were determined in a gentamicin protection assay. The graphs show the percentages of adhesion and invasion of inhibitor-treated cells, relative to control cells (means 盨D of three independent experiments performed in duplicate). *, P < 0.05.
S1056	AC480 (BMS-599626) AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.	Genome Med, 2020, 18;12(1):17 PLoS Genet, 2016, 12(9):e1006279 Asian J Androl, 2016, 10.4103/1008-682X	Co-treatments of PI-103 and EGFR inhibitors enhance cytotoxicity in SUM149PT cells. Cells were treated with 0.3 uM of PI-103 in combination with different concentrations (0.1 and 1 uM) of EGFR inhibitors (BMS-599626) for -72 hrs. Cell viability was measured by MTT assay as described in Materials and methods. Data from two independent experiments performed in triplicate are shown as mean+SEM. P < 0.05; P < 0.01; **P < 0.001.
S1486	AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.	Genome Med, 2020, 18;12(1):17 Mol Pharmacol, 2019, 95(5):528-536 Oncotarget, 2019, 10(68):7185-7197	EGFR-SGLT1 interaction is irresponsive to modulators of EGFR’s tyrosine kinase. A: Immunoprecipitation coupled Western blot analysis ofinteractionsbetween EGFR-HA and SGLT1-FlaginHEK293 cells treatedwith EGF or AEE788. EGFR, total EGFR; pEGFR, phosphorylated EGFR; IP, immunoprecipitation; IB, immunoblot. Input, expression levels of indicated exogenous proteinsin HEK293 whole celllysates used for the IP.
S7000	AP26113-analog (ALK-IN-1) AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.	Clin Cancer Res, 2015, 21(1):166-74 Clin Cancer Res, 2014, 20(22):5686-96 Jpn J Clin Oncol, 2014, 44(10):963-8	Several ALK inhibitors effectively inhibit the growth of CD74–ROS1–addicted Ba/F3 cells. A, Ba/F3 cells expressing CD74–ROS1 (clone #6) were seeded in 96-well plates and treated with the indicated concentration of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 72 hours. Cell viability was analyzed using the CellTiter-Glo Assay. B, IC50 values (nmol/L) of Ba/F3 cell lines expressing CD74–ROS1 (clone #6) against various ALK inhibitors are shown. Average IC50 values against crizotinib, ceritinib, or AP26113 were calculated from the three independent experiments. IC50 values against ASP3026 and alectinib were calculated from the single experiment. C, inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74–ROS1–expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 3 hours. Cell lysates were immunoblotted to detect the indicated proteins.
S2205	OSI-420 OSI-420 (DesMethyl Erlotinib, CP-473420) is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).	J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1166:122554 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8	Mean plasma concentration vs. time after single-dose oral administration of CCB and ERT in six Wistar rats.
S1170	WZ3146 WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).	Aging (Albany NY), 2020, 12(19):19022-19044	T47D cells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of WZ3146 for 24 hours.
S2752	HER2-Inhibitor-1 HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.		confluent 10cm plates, 24hour FBS starvation, then treatment with compounds at 10nM for 30mins, followed by 5 minutes of 0.05ug/ml of EGF. Pellet was sonicated (setting 5, 5 seconds, twice), then quenched with 2XGSB. Loaded 10ul on AnyKD BioRad gel (20mins at 250V), transfered with BioRad Turbo system for 15 minutes (1.5A, 25V). Blocked with 5% milk for 1 hour at RT. Rocked overnight at 1:1000 in 5% BSA with primary Abs; Anti-rabbit secondary Ab at 1:2000 in 5% milk for 1 hour, developed with Thermo Femto Kit.
S1179	WZ8040 WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).	Biochemistry, 2018, 57(8):1369-1379 Nat Commun, 2016, 7:10690	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WZ8040 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S2185	Allitinib (AST-1306) Allitinib (AST-1306, AST-6) is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.	Front Cell Dev Biol, 2020, 8:605110 Cell Signal, 2020, 65:109439 Life Sci, 2020, 15;251:117634	Reversal effect of AST-1306 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without AST-1306. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line.
S7284	Rociletinib (CO-1686) Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with K_i of 21.5 nM and 303.3 nM for EGFR^L858R/T790M and EGFR^WT in cell-free assays, respectively. Phase 2.	Genome Med, 2020, 18;12(1):17 Mol Oncol, 2020, 14(6):1152-1169 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Western blot analysis of H1975 mock and H1975 EGFR cells treated with the indicated concentrations of EGF and rociletinib for phosphorylated (p-) and total (t-) EGFR, AKT, ERK1/2, and b-actin.
S1342	Genistein (NPI 031L) Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.	Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z Theranostics, 2021, 11(5):2364-2380 Theranostics, 2021, 11(5):2364-2380
S2755	Varlitinib Varlitinib (ARRY334543) is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.	Pharmaceutics, 2019, 11(11) Pharmaceutics, 2018, 10(3) Oncol Rep, 2018, 40(2):635-646
S2922	Icotinib (BPI-2009H) Icotinib (BPI-2009H) is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).	Nat Cell Biol, 2019, 21(8):1027-1040 Oncogene, 2017, 36(45):6235-6243 Oral Oncology, 2016, 10.1016/j.oraloncology.2016.05.010	B. Effect of Icotinib treatment on the subcellular localization of ABCG2 in NCI-H460/MX20 cell. ABCG2 staining is shown in green. DAPI (blue) counterstains the nuclei. C. Effect of Icotinib on the ATPase activity of ABCG2: The BeFx-sensitive specific ATPase activity of ABCG2 was determined in the presence of 0-5 μM of Icotinib as described in supplemental methods. The activity in the absence of Icotinib (basal activity) was considered to be 100%, and % -fold stimulation ± S.D. (Y-axis) was plotted as a function of indicated concentrations of Icotinib (X-axis). D. Effect of Icotinib on the photolabeling of ABCG2 with [125I]-IAAP: Crude membranes from ABCG2 expressing MCF7-FLV1000 cells were photo-crosslinked with [125I]-IAAP in the presence and absence of 0-50 μM of Icotinib as described in supplemental methods. [125I]-IAAP incorporated in ABCG2 band was quantified using ImageQuant software and plotted as % [125I]-IAAP incorporated ± S.D. (Y-axis) as a function of varying concentration of Icotinib (X-axis). The upper panel shows a representative autoradiogram from three independent experiments and the arrow represents the ABCG2 band photo-crosslinked with [125I]-IAAP.
S2784	TAK-285 TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.	Oncotarget, 2020, 11(46):4224-4242 Mol Pharmacol, 2019, 95(5):528-536 Sci Signal, 2018, 11(549)
S2867	WHI-P154 WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.	J Med Chem, 2020, 31 Carcinogenesis, 2020, 41(7):993-1004 Int J Med Sci, 2020, 17(18):3065-3072	Reversal effect of WHI-P154 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without WHI-P154. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line.
S2554	Daphnetin Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.	Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7 Int Immunopharmacol, 2019, 72:195-203 Inflamm Res, 2017, 66(7):579-589	C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
S7039	PD168393 PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.	Int J Biochem Cell Biol, 2019, 115:105578 Theranostics, 2017, 7(3):664-676 Oncotarget, 2016,	(B) Immunohistochemical staining for α-actinin and EdU showed that EGFR inhibitor (PD-168393), JNK inhibitor (sp-600125), and SP-1 inhibitor (mithramycin A) could abolish the effect of TIMP-3 siRNA in promoting cardiomyocyte proliferation. n=3 per group for Western blot. At least 2000 cells were quantified in each group. Data are shown as mean±SEM and reflect at least three independent experiments. Scale bar: 100 μm. , P<0.05, **, P<0.001 versus respective control.
S2895	Tyrphostin 9 Tyrphostin 9 (SF 6847, RG-50872) is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.
S7206	CNX-2006 CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.	Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w Cancer Sci, 2016, 107(4):461-8	d) Western blots for phosphorylation of epidermal growth factor receptor (EGFR) and MET, cleaved PARP as an apoptotic marker, and b-actin in HCC827 and their resistant clones. Total cell lysates were extracted 24 h after exposure of DMSO, 0.5 μM erlotinib, 0.5 μM CNX-2006, PHA-665752 and their combinations.
S8009	AG-18 AG-18 (RG-50810, Tyrphostin A23, TX 825) inhibits EGFR with IC50 of 35 μM.	Reproduction, 2016, 151(2):179-85
S0711	Canertinib dihydrochloride Canertinib (CI-1033, PD-183805, compound 18) dihydrochloride is a potent and irreversible inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. Canertinib dihydrochloride inhibits cellular EGFR and ErbB2 autophosphorylation with IC50 of 7.4 nM and 9 nM, respectively.	Acta Physiol (Oxf), 2021, 10.1111/apha.13661 Sci Rep, 2017, BMC Cancer, 2017,
S6525	AG 555 AG-555 (Tyrphostin B46) is an inhibitor of tyrosine kinase, interacts directly with topoisomerase I, thus preventing DNA relaxation. It inhibits EGFR with an IC50 of 0.7 μM.
S7298	AZ5104 AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.	J Pharm Biomed Anal, 2020, 177:112871 Clin Cancer Res, 2019, 25(8):2575-2587 Sci Rep, 2019, 9(1):5309
S8724	Lazertinib Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.	Mol Cancer Ther, 2018, 17(10):2257-2265
S7297	Osimertinib (AZD9291) Osimertinib (AZD9291, Mereletinib) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.	Nat Commun, 2021, 12(1):2346 Cell Rep, 2021, 34(3):108647 Mol Cancer, 2021, 20(1):17	Western blot analysis for total (t-) and phosphorylated (p-) EGFR, AKT, ERK1/2, and β actin in H1975 parental and resistant (COR#3, AZDR#1) cells.
S7557	CL-387785 (EKI-785) CL-387785 (EKI-785, WAY-EKI 785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.	J Biol Chem, 2017, 292(24):10112-10122 Nature, 2017, 550(7675):270-274 Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2789	C, EGFR L718Q and L844V Ba/F3 cells retain sensitivity to irreversible quinazoline EGFR inhibitors. Cells were treated with different drugs at the indicated concentrations, and viable cells were measured after 72 hours of treatment and plotted relative to untreated controls. For Western blot analysis, 3T3 cells expressing the respective constructs were treated with different drugs at indicated concentrations for 16 hours. Cell extracts were immunoblotted to detect the indicated proteins. D, EGFR Del 1/L718Q Ba/F3 cells have a growth disadvantage. Equal number of cells was seeded in the presence of or absence of EGF or IL3. Cell number was evaluated in triplicate at the indicated time points.
S6509	AG 494 AG-494, a member of the tyrphostin family of tyrosine kinase inhibitors, is a potent inhibitor of EGF receptor autophosphorylation (IC50=1.2 μM) and EGF-dependent cell growth (IC50=6 μM).
S8362	Tucatinib (Irbinitinib, ONT-380) Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.	Cancer Discov, 2020, 10(5):674-687 Nat Cell Biol, 2019, 21(8):1027-1040 Sci Signal, 2019, 12(565)
S8294	Olmutinib (BI 1482694) Olmutinib (BI 1482694) is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton's tyrosine kinase.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Sci Rep, 2019, J Thorac Oncol, 2019, 14(9):1556-1566
S6523	RG14620 RG14620 (Tyrphostin RG14620), an EGFR inhibitor of the tyrphostin family, directly inhibits the transport function of ABCG2/BCRP.
S6546	PD153035 PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM).	Nature, 2021, 10.1038/s41586-020-03085-8 Int J Mol Sci, 2021, 22(8)3945 FEBS Lett, 2021, 595(5):563-576
S6541	MTX-211 MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase.
S6813	Mobocertinib (TAK788) Mobocertinib (TAK788, AP32788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent.	Lung Cancer, 2020, 152:135-142
S2250	(-)-Epigallocatechin Gallate (-)-Epigallocatechin Gallate(EGCG) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.	Molecules, 2021, 26(5)1210 Odontology, 2021, 10.1007/s10266-021-00597-1 PLoS Negl Trop Dis, 2020, 17;14(4):e0008224
S7786	Erlotinib (OSI-774) Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.	Nat Cell Biol, 2021, 23(4):377-390 Sci Adv, 2021, 7(10)eabe8671 Proc Natl Acad Sci U S A, 2021, 118(19)e2019580118	Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone.
S0070	Gefitinib-based PROTAC 3 Gefitinib-based PROTAC 3 which conjugates an EGFR binding element to a VHL ligand via a linker induces degradation of EGFR and mutants with DC50 of 11.7 nM and 22.3 nM in HCC827(Exon 19 del) and H3255 (L858R) cells, respectively.
S5098	Gefitinib hydrochloride Gefitinib (ZD1839) is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively.	Nat Cell Biol, 2021, 23(4):377-390 Mol Cancer, 2021, 20(1):17 Cancers (Basel), 2021, 13(2)E272
S7810	Afatinib (BIBW2992) Dimaleate Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.	Nat Cell Biol, 2021, 23(4):377-390 Theranostics, 2021, 11(6):2594-2611 Mol Cancer, 2021, 20(1):17	Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay.
S7971	AZD3759 AZD3759 is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1.	Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7 Clin Cancer Res, 2019, 25(8):2575-2587 Cancer Lett, 2019, 458:29-38
S7358	Poziotinib (HM781-36B) Poziotinib (HM781-36B, NOV120101) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also induces apoptosis and G1 cell cycle arrest. Phase 2.	Thorac Cancer, 2021, 10.1111/1759-7714.13931 Acta Neuropathol, 2020, 17 Clin Cancer Res, 2020, 10.1158/1078-0432
S8229	Brigatinib (AP26113) Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.	EMBO J, 2021, e105784 Sci Signal, 2020, 26;13(633):eaba3176 Oncol Rep, 2020, 44(6):2581-2594	Immunoblotting analysis of H3122 and H3122-CER cells showing that brigatinib did not inhibit EGFR phosphorylation (p-EGFR). Total EGFR (t-EGFR) is also shown. Actin was used as a loading control. The cells were treated with brigatinib for 2 hours.
S5078	Osimertinib mesylate Osimertinib mesylate (AZD9291) is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.	Mol Cancer, 2021, 20(1):17 Transl Lung Cancer Res, 2021, 10(3):1277-1291 Biochim Biophys Acta Mol Cell Res, 2021, 1868(6):119016
S6698	TQB3804 (EGFR-IN-7) TQB3804 (EGFR-IN-7) is a selective and potent EGFR kinase inhibitor with IC50 of 0.46 nM, 0.13 nM, 0.26 nM, 0.19 nM and 1.07 nM for for EGFR^{d746-750/T790M/C797S}, EGFR^{L858R/T790M/C797S}, EGFR^{d746-750/T790M}, EGFR^L858R/T790M and EGFR^WT, respectively. TQB3804 (EGFR-IN-7) shows anti-tumor activity.
S0360	EGFR Inhibitor EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics.
S8412	Naquotinib(ASP8273) Naquotinib (ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.	Expert Opin Emerg Drugs, 2018, 10.1080/14728214.2018.1558203 Share on FacebookShare on TwitterShare on Google+
S2406	Chrysophanic Acid Chrysophanic Acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.	Cell Prolif, 2020, e12871 Naunyn Schmiedebergs Arch Pharmacol, 2019, 10.1007/s00210-019-01746-8	After starved in serum-free medium for 24h, A549 cells incubated with the indicated concentrations of Chrysophanic acid for 3h,followed by 15-minute stimolation of 100ng/ml EGF
S7824	Nazartinib (EGF816) Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Transl Oncol, 2019, 12(5):705-713 J Thorac Oncol, 2019, 14(9):1556-1566
S3759	Norcantharidin Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
S1054	AG99 AG99 (Tyrphostin 46,Tyrphostin A46,Tyrphostin B40) is a potent and selective inhibitor of EGFR.
S0151	AG-1557 AG-1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.
S2115	RG 13022 RG 13022 (Tyrphostin RG13022) inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.
S7926	Lifirafenib (BGB-283) Lifirafenib (BGB-283, Beigene-283) potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.	Nat Commun, 2020, 11(1):3157 Cell Rep, 2020, 31(11):107764 Cell Rep, 2019, 29(3):573-588
S4667	Lidocaine hydrochloride Lidocaine hydrochloride (Lidothesin, Lignocaine, Xyloneural) is an inhibitor of epidermal growth factor receptor (EGFR) and has antiproliferative effect on human tongue cancer cells. Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.	Exp Ther Med, 2021, 21(5):424
S8036	Butein Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR.	Am J Cancer Res, 2020, 10(11):3721-3736 Oncotarget, 2015, 6(14):12637-53
S8242	EAI045 EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.	Pharmazie, 2018, 73(11):630-634
S8814	TAS6417 TAS6417 (CLN-081, TPC-064) is a novel EGFR inhibitor that targets EGFR exon 20 insertion mutations while sparing wild-type (WT) EGFR. IC50 values ranges from 1.1 ± 0.1 to 8.0 ± 1.1 nmol/L.
S9414	Cyasterone Cyasterone is the main phytoecdysteroid component found in Cyathula capitata. It is a natural EGFR inhibitor and maybe a promising anti-cancer agent.
S6809	SU5214 SU5214 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.
S8817	Almonertinib (HS-10296) Almonertinib (HS-10296, Ameile) is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.	Biochem Pharmacol, 2021, 188:114516
S8741	Avitinib (AC0010) Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity.
A2000	Cetuximab (anti-EGFR) Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. MW : 145.781 KD.	Mol Imaging Biol, 2020, 10.1007/s11307-020-01539-z Photochem Photobiol, 2020, 10.1111/php.13231 Nat Commun, 2019, 10(1):2621	Mice showed progression disease to first-line treatment were randomized 1:1 to the two arms of treatment and were treated until onset of progression disease or until the end-time of experiment in case of response (fixed to 52 weeks from the start of first-line therapy ), as indicated in in the Materials and Methods section. Growth curves of HCC827 xenografts treated in secondline with osimertinib plus selumetinib or cetuximab are represented as changes in the values of volumes as percentage compared to baseline tumor volume at the time of progression diasease to first-line (defined as 100%) for each case. Median tumor volume at PD2 was of 348 mm³.
S8312	NSC228155 NSC228155 is an activator of EGFR. It binds to the sEGFR dimerization domain II and modulates EGFR tyrosine phosphorylation.	Cell Death Dis, 2021, 12(2):173 Am J Transl Res, 2020, 12(5):2295-2304
S6530	EBE-A22 EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.

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S1023	Erlotinib HCl (OSI-744) Erlotinib HCl (OSI-744, CP358774, NSC 718781) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.	Nat Cell Biol, 2021, 23(4):377-390 Sci Adv, 2021, 7(10)eabe8671 Proc Natl Acad Sci U S A, 2021, 118(19)e2019580118	Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone.
S1025	Gefitinib (ZD1839) Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.	Nat Cell Biol, 2021, 23(4):377-390 Theranostics, 2021, 11(2):824-840 Theranostics, 2021, 11(6):2594-2611	Perturbation of EGFR by its ligand EGF and gefitinib (ZD-1839 Iressat; inhibits EGFR) produces opposite responses in the predicted EGFR target genes SOCS2 and NR2E1.
S1028	Lapatinib (GW-572016) Ditosylate Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.	Nat Cell Biol, 2021, 23(4):377-390 J Transl Med, 2021, 19(1):184 Cancer Med, 2021, 10(7):2370-2379	Combination of NVP-AEW541 and lapatinib cooperatively inhibits the growth of NVP-AEW541 resistant murine rhabdomyosarcoma primary cell cultures with Igf1r/Her2 complexes. Cell viability assay for Naïve, untreated (U20325; A) and NVP-AEW541 innately resistant mouse rhabdomyosarcoma primary culture (U44676; B) treated with varying concentrations of NVP-AEW541, lapatinib, or a combination of both. Naïve cells (U20325) were sensitive to NVP-AEW541, but lapatinib had no cooperativity. In contrast, NVP-AEW541 at moderate doses increased cell growth in resistant cell cultures (U44676). However, this paradoxical effect was reduced by the addition of lapatinib, although lapatinib treatment alone had very little effect. C, the NVP-AEW541 resistant primary tumor cell line (U44676) was treated with DMSO, 5 μmol/L lapatinib, 5 μmol/L NVP-AEW541, and a combination of 5 μmol/L NVP-AEW541+lapatinib for 25 minutes and Western blot analysis was done on lysates for p-Igf1r and p-Her2.
S1011	Afatinib (BIBW2992) Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.	Cancer Cell, 2021, S1535-6108(20)30609-7 Nat Cell Biol, 2021, 23(4):377-390 Cancer Res, 2021, canres.2276.2020	Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay.
S1006	Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.	Int J Cancer, 2021, 10.1002/ijc.33606 Oncogene, 2021, 40(14):2567-2580 FASEB J, 2021, 35(5):e21598	C and D, in vivo subcutaneous tumor growth curves (C) and tumor weight quantification of intersected subcutaneous tumor tissues (D) of Huh7 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n =18). , P < 0.05. E and F,in vivo subcutaneous tumor growth curves (E) and tumor weight quantification of intersected subcutaneous tumor tissues (F) of SK-Hep1 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n = 18). , P < 0.05.
S9786^新	BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
S6899^新	Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and MET activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S6897^新	Epertinib hydrochloride Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.
S8584^新	Theliatinib (HMPL-309) Theliatinib (HMPL-309) is a highly potent EGFR inhibitor with Ki value of 0.05 nM against the wild type EGFR and IC50 values of 3 nM and 22 nM against EGFR and EGFR T790M/L858R mutant. It demonstrats 50 fold greater selectivity for EGFR compared to 72 other kinases.
S6868^新	Alflutinib (AST2818) mesylate Alflutinib (AST2818) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.
S8920^新	(Rac)-JBJ-04-125-02 JBJ-04-125-02 is a mutant-selective allosteric inhibitor of EGFR.
S8852^新	Pyrotinib (SHR-1258) dimaleate Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.	Clin Transl Med, 2020, 10(8):e254
S6805^新	Tyrphostin AG-528 Tyrphostin AG-528 (Tyrphostin B66) is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity.
S1046	Vandetanib (ZD6474) Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).	J Clin Endocrinol Metab, 2021, dgab020 Drug Metab Dispos, 2021, 49(1):53-61 J Enzyme Inhib Med Chem, 2021, 36(1):163-174	Vandetanib reduced extracellular nitrite levels in endothelial cells. MS1 endothelial cells (ECs) were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]), 50 ng/mL of vascular endothelial growth factor (VEGF) or matched vehicle (PBS; 0.5 hours), and L-arginine and soluble N-ethylmaleamide sensitive factor attachment protein (SNAP) added (1.5 hours). Vandetanib lowered nitrite levels in MS1 Ecs (P0.0003). VEGF was used a positive control and increased nitrite levels (*P0.02). These findings indicate that vandetanib lowered endothelial cell NO levels.
S2150	Neratinib (HKI-272) Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.	Cancer Med, 2021, 10(7):2370-2379 Cancer Cell, 2020, 37(2):183-199 Acta Neuropathol, 2020, 17	HER2 mutations V777L, D769H, V842I, G309A induce gain-of-function over HER2 WT in MCF10A mammary epithelial cells. B, HER2 WT, L755S, and del.755–759 cells were grown in Matrigel in the presence of DMSO vehicle (0.5%), neratinib (0.5 μmol/L) or gefitinib (0.5 μmol/L). Phase contrast images were obtained as in A. C, MCF10A-HER2 WT or mutants were seeded in soft agar. After 7 days of growth, they were treated with DMSO vehicle (0.5%), lapatinib (0.5 μmol/L) or neratinib (0.5 μmol/L) for an additional week. Error bars represent 95% highest posterior density intervals. *, Significant difference between the HER2 mutant and HER2 WT; #, the effect of inhibitor treatment was significant (95% highest posterior density interval did not contain 0 for both). D, photomicrographs of the colonies in soft agar on day 12, magnification ×40.
S1019	Canertinib (CI-1033) Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3.	Acta Physiol (Oxf), 2021, 10.1111/apha.13661 ACS Chem Biol, 2021, 10.1021/acschembio.0c01000 Genome Med, 2020, 18;12(1):17	(B–C) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 lg). The cells were then treated with Erlotinib (20 lM), Gefitinib (20 lM), Lapatinib (20 lM), CI-1033 (8 lM), LY294002 (20 lM) and Bortezomib (20 lM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (±SD) of duplicate values of a representative experiment that was independently repeated for five times.
S2111	Lapatinib (GW-572016) Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.	Nat Cell Biol, 2021, 23(4):377-390 Mol Cell, 2021, 81(4):708-723.e5 Cell Rep, 2021, 34(10):108822	Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using speciﬁc antibodies.
S1143	AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42, Zinc02557947) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.	Front Nutr, 2021, 8:649640 Oncol Rep, 2021, 10.3892/or.2021.7926 Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7	IL6 normally induces WASF3 expression in MDA231 cells, but co-treatments with AG490 (a pan-JAK inhibitor) show a dose-dependent reduction of both WASF3 levels and activated STAT3 levels.
S1167	CP-724714 CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.	Int J Mol Sci, 2020, 22(1)E82 NPJ Breast Cancer, 2020, 6:30 Cancers (Basel), 2019, 11(3)
S2727	Dacomitinib (PF-00299804) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2.	Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w Nat Commun, 2020, 11(1):4607 Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2321
S1173	WZ4002 WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM in BaF3 cell line; does not inhibit ERBB2 phosphorylation (T798I).	Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w Cell Res, 2020, 10.1038/s41422-020-00409-1 Cancer Res, 2020, 80(21):4655-4667	Antitum o r activity of WZ4002 and/or E7050 in mouse xenograft models of human tumors. SCID mice-bearing PC-9/Vec (A), PC-9/HGF#5 (B), H1975 (C), or HCC827ER (D) tumors were administered 25 mg/kg WZ4002 and/or E7050 once daily for 14 to 21 days. Tumor volume was measured using calipers on the indicated days. Mean?SE tumor volumes are shown for groups of 4 to 5 mice.
S2192	Sapitinib (AZD8931) Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.	Nature, 2020, 584(7822):608-613 Nature, 2020, 584(7822):608-613 J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X
S1194	CUDC-101 CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.	Cancer Sci, 2020, 112(1):133-143 Anticancer Drugs, 2020, 31(2):158-168 NPJ Breast Cancer, 2020, 6:30	(a) Decay-corrected microPET/CT scan of MDA-MB-231 tumor bearing mice (n = 4) at 2, 4, and 24 h after i.v. injection of [64Cu]7. The image obtained with coinjection of CUDC-101 (20 mg/kg body weight) is shown for a 24 h blockade. Tumors are indicated by arrows. (b) Decay-corrected region-of interest (ROI) analysis on microPET images of the tumor uptake of [64Cu]7 with or without coinjection of CUDC-101 (20 mg/kg body weight). , P < 0.05; *, P < 0.01.
S2728	AG-1478 (Tyrphostin AG-1478) AG-1478 (Tyrphostin AG-1478, NSC 693255) is a selective EGFR inhibitor with IC50 of 3 nM in cell-free assays, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR. AG-1478 (Tyrphostin AG-1478) inhibits encephalomyocarditis virus (EMCV) and hepatitis c virus (HCV) by targeting phosphatidylinositol 4-kinase IIIα (PI4KA).	Theranostics, 2021, 11(3):996-1015 Oncogenesis, 2021, 10(3):25 Am J Transl Res, 2021, 13(2):708-718	A549 cells were treated with G15 (a specific antagonist of GPR30, 1 uM), AG1478 (a potent antagonist of EGFR, 10 uM), BPA (10^-5 M) alone for 15 min or BPA after a 90-min pretreatment with G15 or AG1478 for 15 min. Then the expression of p-ERK1/2 and total ERK1/2 were measured by western blot analysis.
S1079	PD153035 HCl PD153035 HCl (SU-5271 HCl, AG1517 HCl, ZM 252868 HCl) is a potent and specific inhibitor of EGFR with K_i and IC50 of 5.2 pM and 29 pM in cell-free assays; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.	Int J Mol Sci, 2021, 22(8)3945 FEBS Lett, 2021, 595(5):563-576 FEBS Lett, 2021, 10.1002/1873-3468.14032	IGF-1 and IL-1β mediated induction of Bcl-2 expression involves EGFR. (A) Bcl-2 mRNA levels in AALEBs treated with IGF-1 or IL-1β in the presence or absence of two EGFR tyrosine kinase inhibitors, EKB-569 (1 μM) or PD153035 (1 μM).
S1392	Pelitinib (EKB-569) Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Pelitinib (EKB-569) also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282 nM, 800 nM and 1255 nM, respectively. Phase2.	Mol Cancer Ther, 2020, 5;molcanther.1131.2019 Nat Cell Biol, 2019, 21(6):778-790 Korean J Parasitol, 2017, 55(5):491-503	HBMEC were preincubated with the indicated concentrations of either ErB1/2/4 inhibitor (Pelitinib; EKB-569), and cells were then infected for 4 h with the unencapsulated strain, MC58 siaD. The numbers of adherent (black bars) and invasive (gray bars) bacteria were determined in a gentamicin protection assay. The graphs show the percentages of adhesion and invasion of inhibitor-treated cells, relative to control cells (means 盨D of three independent experiments performed in duplicate). *, P < 0.05.
S1056	AC480 (BMS-599626) AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.	Genome Med, 2020, 18;12(1):17 PLoS Genet, 2016, 12(9):e1006279 Asian J Androl, 2016, 10.4103/1008-682X	Co-treatments of PI-103 and EGFR inhibitors enhance cytotoxicity in SUM149PT cells. Cells were treated with 0.3 uM of PI-103 in combination with different concentrations (0.1 and 1 uM) of EGFR inhibitors (BMS-599626) for -72 hrs. Cell viability was measured by MTT assay as described in Materials and methods. Data from two independent experiments performed in triplicate are shown as mean+SEM. P < 0.05; P < 0.01; **P < 0.001.
S1486	AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.	Genome Med, 2020, 18;12(1):17 Mol Pharmacol, 2019, 95(5):528-536 Oncotarget, 2019, 10(68):7185-7197	EGFR-SGLT1 interaction is irresponsive to modulators of EGFR’s tyrosine kinase. A: Immunoprecipitation coupled Western blot analysis ofinteractionsbetween EGFR-HA and SGLT1-FlaginHEK293 cells treatedwith EGF or AEE788. EGFR, total EGFR; pEGFR, phosphorylated EGFR; IP, immunoprecipitation; IB, immunoblot. Input, expression levels of indicated exogenous proteinsin HEK293 whole celllysates used for the IP.
S7000	AP26113-analog (ALK-IN-1) AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.	Clin Cancer Res, 2015, 21(1):166-74 Clin Cancer Res, 2014, 20(22):5686-96 Jpn J Clin Oncol, 2014, 44(10):963-8	Several ALK inhibitors effectively inhibit the growth of CD74–ROS1–addicted Ba/F3 cells. A, Ba/F3 cells expressing CD74–ROS1 (clone #6) were seeded in 96-well plates and treated with the indicated concentration of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 72 hours. Cell viability was analyzed using the CellTiter-Glo Assay. B, IC50 values (nmol/L) of Ba/F3 cell lines expressing CD74–ROS1 (clone #6) against various ALK inhibitors are shown. Average IC50 values against crizotinib, ceritinib, or AP26113 were calculated from the three independent experiments. IC50 values against ASP3026 and alectinib were calculated from the single experiment. C, inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74–ROS1–expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 3 hours. Cell lysates were immunoblotted to detect the indicated proteins.
S2205	OSI-420 OSI-420 (DesMethyl Erlotinib, CP-473420) is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).	J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1166:122554 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8	Mean plasma concentration vs. time after single-dose oral administration of CCB and ERT in six Wistar rats.
S1170	WZ3146 WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).	Aging (Albany NY), 2020, 12(19):19022-19044	T47D cells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of WZ3146 for 24 hours.
S2752	HER2-Inhibitor-1 HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.		confluent 10cm plates, 24hour FBS starvation, then treatment with compounds at 10nM for 30mins, followed by 5 minutes of 0.05ug/ml of EGF. Pellet was sonicated (setting 5, 5 seconds, twice), then quenched with 2XGSB. Loaded 10ul on AnyKD BioRad gel (20mins at 250V), transfered with BioRad Turbo system for 15 minutes (1.5A, 25V). Blocked with 5% milk for 1 hour at RT. Rocked overnight at 1:1000 in 5% BSA with primary Abs; Anti-rabbit secondary Ab at 1:2000 in 5% milk for 1 hour, developed with Thermo Femto Kit.
S1179	WZ8040 WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).	Biochemistry, 2018, 57(8):1369-1379 Nat Commun, 2016, 7:10690	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WZ8040 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S2185	Allitinib (AST-1306) Allitinib (AST-1306, AST-6) is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.	Front Cell Dev Biol, 2020, 8:605110 Cell Signal, 2020, 65:109439 Life Sci, 2020, 15;251:117634	Reversal effect of AST-1306 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without AST-1306. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line.
S7284	Rociletinib (CO-1686) Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with K_i of 21.5 nM and 303.3 nM for EGFR^L858R/T790M and EGFR^WT in cell-free assays, respectively. Phase 2.	Genome Med, 2020, 18;12(1):17 Mol Oncol, 2020, 14(6):1152-1169 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Western blot analysis of H1975 mock and H1975 EGFR cells treated with the indicated concentrations of EGF and rociletinib for phosphorylated (p-) and total (t-) EGFR, AKT, ERK1/2, and b-actin.
S1342	Genistein (NPI 031L) Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.	Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z Theranostics, 2021, 11(5):2364-2380 Theranostics, 2021, 11(5):2364-2380
S2755	Varlitinib Varlitinib (ARRY334543) is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.	Pharmaceutics, 2019, 11(11) Pharmaceutics, 2018, 10(3) Oncol Rep, 2018, 40(2):635-646
S2922	Icotinib (BPI-2009H) Icotinib (BPI-2009H) is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).	Nat Cell Biol, 2019, 21(8):1027-1040 Oncogene, 2017, 36(45):6235-6243 Oral Oncology, 2016, 10.1016/j.oraloncology.2016.05.010	B. Effect of Icotinib treatment on the subcellular localization of ABCG2 in NCI-H460/MX20 cell. ABCG2 staining is shown in green. DAPI (blue) counterstains the nuclei. C. Effect of Icotinib on the ATPase activity of ABCG2: The BeFx-sensitive specific ATPase activity of ABCG2 was determined in the presence of 0-5 μM of Icotinib as described in supplemental methods. The activity in the absence of Icotinib (basal activity) was considered to be 100%, and % -fold stimulation ± S.D. (Y-axis) was plotted as a function of indicated concentrations of Icotinib (X-axis). D. Effect of Icotinib on the photolabeling of ABCG2 with [125I]-IAAP: Crude membranes from ABCG2 expressing MCF7-FLV1000 cells were photo-crosslinked with [125I]-IAAP in the presence and absence of 0-50 μM of Icotinib as described in supplemental methods. [125I]-IAAP incorporated in ABCG2 band was quantified using ImageQuant software and plotted as % [125I]-IAAP incorporated ± S.D. (Y-axis) as a function of varying concentration of Icotinib (X-axis). The upper panel shows a representative autoradiogram from three independent experiments and the arrow represents the ABCG2 band photo-crosslinked with [125I]-IAAP.
S2784	TAK-285 TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.	Oncotarget, 2020, 11(46):4224-4242 Mol Pharmacol, 2019, 95(5):528-536 Sci Signal, 2018, 11(549)
S2867	WHI-P154 WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.	J Med Chem, 2020, 31 Carcinogenesis, 2020, 41(7):993-1004 Int J Med Sci, 2020, 17(18):3065-3072	Reversal effect of WHI-P154 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without WHI-P154. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line.
S2554	Daphnetin Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.	Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7 Int Immunopharmacol, 2019, 72:195-203 Inflamm Res, 2017, 66(7):579-589	C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
S7039	PD168393 PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.	Int J Biochem Cell Biol, 2019, 115:105578 Theranostics, 2017, 7(3):664-676 Oncotarget, 2016,	(B) Immunohistochemical staining for α-actinin and EdU showed that EGFR inhibitor (PD-168393), JNK inhibitor (sp-600125), and SP-1 inhibitor (mithramycin A) could abolish the effect of TIMP-3 siRNA in promoting cardiomyocyte proliferation. n=3 per group for Western blot. At least 2000 cells were quantified in each group. Data are shown as mean±SEM and reflect at least three independent experiments. Scale bar: 100 μm. , P<0.05, **, P<0.001 versus respective control.
S2895	Tyrphostin 9 Tyrphostin 9 (SF 6847, RG-50872) is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.
S7206	CNX-2006 CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.	Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w Cancer Sci, 2016, 107(4):461-8	d) Western blots for phosphorylation of epidermal growth factor receptor (EGFR) and MET, cleaved PARP as an apoptotic marker, and b-actin in HCC827 and their resistant clones. Total cell lysates were extracted 24 h after exposure of DMSO, 0.5 μM erlotinib, 0.5 μM CNX-2006, PHA-665752 and their combinations.
S8009	AG-18 AG-18 (RG-50810, Tyrphostin A23, TX 825) inhibits EGFR with IC50 of 35 μM.	Reproduction, 2016, 151(2):179-85
S0711	Canertinib dihydrochloride Canertinib (CI-1033, PD-183805, compound 18) dihydrochloride is a potent and irreversible inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. Canertinib dihydrochloride inhibits cellular EGFR and ErbB2 autophosphorylation with IC50 of 7.4 nM and 9 nM, respectively.	Acta Physiol (Oxf), 2021, 10.1111/apha.13661 Sci Rep, 2017, BMC Cancer, 2017,
S6525	AG 555 AG-555 (Tyrphostin B46) is an inhibitor of tyrosine kinase, interacts directly with topoisomerase I, thus preventing DNA relaxation. It inhibits EGFR with an IC50 of 0.7 μM.
S7298	AZ5104 AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.	J Pharm Biomed Anal, 2020, 177:112871 Clin Cancer Res, 2019, 25(8):2575-2587 Sci Rep, 2019, 9(1):5309
S8724	Lazertinib Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.	Mol Cancer Ther, 2018, 17(10):2257-2265
S7297	Osimertinib (AZD9291) Osimertinib (AZD9291, Mereletinib) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.	Nat Commun, 2021, 12(1):2346 Cell Rep, 2021, 34(3):108647 Mol Cancer, 2021, 20(1):17	Western blot analysis for total (t-) and phosphorylated (p-) EGFR, AKT, ERK1/2, and β actin in H1975 parental and resistant (COR#3, AZDR#1) cells.
S7557	CL-387785 (EKI-785) CL-387785 (EKI-785, WAY-EKI 785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.	J Biol Chem, 2017, 292(24):10112-10122 Nature, 2017, 550(7675):270-274 Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2789

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EGFR

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EGFR製品