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
S1019	Canertinib (CI-1033)	<1 mg/mL	2 mg/mL	9 mg/mL
S8814	TAS6417	<1 mg/mL	79 mg/mL	79 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
S8817	HS-10296	<1 mg/mL	100 mg/mL	6 mg/mL
S8584	Theliatinib (HMPL-309)	-1 mg/mL	47 mg/mL	-1 mg/mL
S2111	Lapatinib	<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 (PF299804, PF299)	<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	AST-1306	<1 mg/mL	124 mg/mL	<1 mg/mL
S7284	Rociletinib (CO-1686, AVL-301)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1342	Genistein	<1 mg/mL	54 mg/mL	2 mg/mL
S2755	Varlitinib	<1 mg/mL	6 mg/mL	<1 mg/mL
S2922	Icotinib	<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
S7298	AZ5104	<1 mg/mL	97 mg/mL	23 mg/mL
S8724	Lazertinib (YH25448,GNS-1480)	<1 mg/mL	4 mg/mL	<1 mg/mL
S7297	AZD9291	<1 mg/mL	99 mg/mL	43 mg/mL
S7557	CL-387785 (EKI-785)	<1 mg/mL	63 mg/mL	<1 mg/mL
S8294	Olmutinib (HM61713, BI 1482694)	<1 mg/mL	97 mg/mL	23 mg/mL
S2250	(-)-Epigallocatechin Gallate	23 mg/mL	72 mg/mL	83 mg/mL
S7786	Erlotinib	<1 mg/mL	78 mg/mL	15 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
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, NVS-816)	<1 mg/mL	99 mg/mL	99 mg/mL
S3759	Norcantharidin	-1 mg/mL	33 mg/mL	-1 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
S9414	Cyasterone	-1 mg/mL	100 mg/mL	-1 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

亜型選択性的な製品

EGFR製品

All (64) EGFR阻害剤(63) EGFR活性剤(1) 新EGFR製品

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
A2000	Cetuximab 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.	Nat Commun, 2019, 10(1):2621 Cancers (Basel-, 2019, 11(1) Oncogenesis, 2019, 8(10):54	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.
S1023	Erlotinib HCl (OSI-744) Erlotinib HCl (OSI-744) 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.	Cell, 2019, 178(4):807-819.e21 Nat Immunol, 2019, 20(7):835-851 Gastroenterology, 2019, 156(6):1788-1804	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.	Cancer Discov, 2019, 9(7):926-943 Cell Stem Cell, 2019, 25(1):69-86 Nat Cell Biol, 2019, 21(6):778-790	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.	Cell Rep, 2019, 28(9):2331-2344 J Clin Med, 2019, 8(12) Cell Metab, 2018, 28(6):817-832	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) 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 in cell-free assays, respectively.	Nature, 2019, 571(7763):127-131 Nat Med, 2019, 25(1):111-118 Cancer Discov, 2019, 9(7):926-943	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.
S1019	Canertinib (CI-1033) Canertinib (CI-1033) 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.	Mol Oncol, 2019, 13(9):1959-1975 Dev Biol, 2019, 10.1016/j.ydbio.2019.10.006 Nat Methods, 2018, 15(8):631-639	(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.
S8814^新	TAS6417 TAS6417 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.
S6546^新	PD153035 PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM).	Nat Commun, 2019, 10(1):2297 Sci Rep, 2017, 7:44089 Cell Rep, 2016, 14(4):772-781
S6541^新	MTX-211 MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase.
S8817^新	HS-10296 HS-10296 is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
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.
S2111	Lapatinib Lapatinib, 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.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Nat Cell Biol, 2019, 21(8):1027-1040 Clin Cancer Res, 2019, 25(5):1639-1649	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) 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.	Cancer Discov, 2019, 9(6):756-777 Aging (Albany NY), 2019, 11(17):6674-6690 Cancer Cell Int, 2019, 19:57	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.	Cancers (Basel), 2019, 11(3) BMC Cancer, 2018, 18(1):238 Am J Transl Res, 2018, 10(7):2055-2067
S2727	Dacomitinib (PF299804, PF299) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay, effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Phase 2.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 J Thorac Oncol, 2019, 10.1016/j.jtho.2019.09.195 Clin Cancer Res, 2019, 25(2):641-651
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 Cell Biol, 2019, 21(8):1027-1040 Oncogene, 2019, 38(37):6399-6413 Clin Cancer Res, 2018, 24(13):3126-3136	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.	Gut, 2019, 68(6):1024-1033 Nat Commun, 2019, 10(1):2919 Cell Rep, 2019, 26(1):65-78
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 Res, 2019, 79(1):209-219 Int J Mol Sci, 2019, 20(13) Mol Pharmacol, 2019, 95(5):528-536	(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) 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.	Cell Death Dis, 2019, 10(3):191 Mol Cancer Res, 2019, 17(5):1195-1206 J Steroid Biochem Mol Biol, 2019, 187:58-67	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 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.	Oncotarget, 2016, 7(24):36168-36184 Oncogene, 2015, 10.1038/onc.2015.59 Int J Clin Exp Pathol, 2014, 7(11):7663-7671	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. Phase2.	Nat Cell Biol, 2019, 21(6):778-790 Korean J Parasitol, 2017, 55(5):491-503 Pathol Oncol Res, 2015, 10.1007/s12253-015-9916-9	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.	Asian J Androl, 2016, 10.4103/1008-682X Oncotarget, 2016, 7(24):36956-36970 Genes Cancer, 2014, 5(7-8):261-72	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.	Mol Pharmacol, 2019, 95(5):528-536 Oncogenesis, 2018, 7(1):5 Oncotarget, 2017, 8(14):22414-22432	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 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).	Transl Oncol, 2018, 11(6):1406-1418 Transl Lung Cancer Res, 2017, 6(5):600-610 Oncotarget, 2017, 8(58):98771-98781	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).		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).	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	AST-1306 AST-1306 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.	Cell Signal, 2020, 65:109439 Cell Rep, 2019, 28(9):2331-2344 Biochem Biophys Res Commun, 2018, 504(2):427-433	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, AVL-301) 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.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Nat Med, 2018, 24(5):638-646 Nat Commun, 2018, 9(1):4655	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 Genistein, 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.	Mol Cell, 2019, 75(6):1103-1116.e9 Cancer Manag Res, 2018, 10:6205-6216 Drug Deliv, 2018, 25(1):1258-1265
S2755	Varlitinib Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.	Pharmaceutics, 2018, 10(3) Oncol Rep, 2018, 40(2):635-646 Cancer Genet, 2017, 216-217:128-141
S2922	Icotinib Icotinib 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.	Mol Pharmacol, 2019, 95(5):528-536 Sci Signal, 2018, 11(549) Nat Chem Biol, 2016, 12(11):923-930
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.	Biol Open, 2018, 7(1) J Mol Med, 2018, 10.1007/s00109-018-1724-8 Oncol Rep, 2017, 37(1):66-76	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.	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.	Theranostics, 2017, 7(3):664-676	(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 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.	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 inhibits EGFR with IC50 of 35 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 (YH25448,GNS-1480) 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	AZD9291 Osimertinib (AZD9291) 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 Med, 2019, 25(1):111-118 Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Nat Commun, 2019, 10(1):2701	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) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.	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.
S8294	Olmutinib (HM61713, BI 1482694) Olmutinib 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
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.	Oncogene, 2019, 38(15):2690-2705 Onco Targets Ther, 2019, 12:6033-6043 Exp Ther Med, 2018, 15(5):4284-4290
S7786	Erlotinib Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.	Nat Med, 2019, 25(1):111-118 Cell, 2019, 178(4):807-819 Cancer Cell, 2019, 35(3):504-518	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.
S5098	Gefitinib hydrochloride Gefitinib is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively.	Br J Cancer, 2019, 120(3):306-316 Respir Res, 2019, 20(1-:270 Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0248-2
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.	Circulation, 2019, 139(22):2570-2584 Clin Cancer Res, 2018, 24(5):1227-1239 Cancer Discov, 2017, 7(6):575-585	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.	Clin Cancer Res, 2019, 25(8):2575-2587 Cancer Lett, 2019, 458:29-38 Drug Metab Dispos, 2019, 10.1124/dmd.118.084210
S7358	Poziotinib (HM781-36B) Poziotinib (HM781-36B) 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. Phase 2.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Nat Med, 2018, 24(5):638-646 Cancer Cell, 2018, 34(5):807-822
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 ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.	Cell Syst, 2019, 8(2):97-108 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104 Clin Cancer Res, 2018, 24(17):4162-4174	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 is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.	Arch Toxicol, 2019, 10.1007/s00204-019-02453-2 Respir Res, 2019, 20(1-:270 Thorac Cancer, 2019, 10(10):1868-1878
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.	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, NVS-816) 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 Nat Med, 2018, 24(5):638-646
S3759	Norcantharidin Norcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
S7926	Lifirafenib (BGB-283) Lifirafenib (BGB-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.	Cell Rep, 2019, 29(3):573-588 Oncotarget, 2019, 10(23):2237-2251
S4667	Lidocaine hydrochloride Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.
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.
S8242	EAI045 EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
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.
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.
S8312	NSC228155 NSC228155 is an activator of EGFR. It binds to the sEGFR dimerization domain II and modulates EGFR tyrosine phosphorylation.

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A2000	Cetuximab 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.	Nat Commun, 2019, 10(1):2621 Cancers (Basel-, 2019, 11(1) Oncogenesis, 2019, 8(10):54	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.
S1023	Erlotinib HCl (OSI-744) Erlotinib HCl (OSI-744) 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.	Cell, 2019, 178(4):807-819.e21 Nat Immunol, 2019, 20(7):835-851 Gastroenterology, 2019, 156(6):1788-1804	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.	Cancer Discov, 2019, 9(7):926-943 Cell Stem Cell, 2019, 25(1):69-86 Nat Cell Biol, 2019, 21(6):778-790	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.	Cell Rep, 2019, 28(9):2331-2344 J Clin Med, 2019, 8(12) Cell Metab, 2018, 28(6):817-832	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) 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 in cell-free assays, respectively.	Nature, 2019, 571(7763):127-131 Nat Med, 2019, 25(1):111-118 Cancer Discov, 2019, 9(7):926-943	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.
S1019	Canertinib (CI-1033) Canertinib (CI-1033) 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.	Mol Oncol, 2019, 13(9):1959-1975 Dev Biol, 2019, 10.1016/j.ydbio.2019.10.006 Nat Methods, 2018, 15(8):631-639	(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.
S8814^新	TAS6417 TAS6417 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.
S6546^新	PD153035 PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM).	Nat Commun, 2019, 10(1):2297 Sci Rep, 2017, 7:44089 Cell Rep, 2016, 14(4):772-781
S6541^新	MTX-211 MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase.
S8817^新	HS-10296 HS-10296 is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
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.
S2111	Lapatinib Lapatinib, 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.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Nat Cell Biol, 2019, 21(8):1027-1040 Clin Cancer Res, 2019, 25(5):1639-1649	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) 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.	Cancer Discov, 2019, 9(6):756-777 Aging (Albany NY), 2019, 11(17):6674-6690 Cancer Cell Int, 2019, 19:57	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.	Cancers (Basel), 2019, 11(3) BMC Cancer, 2018, 18(1):238 Am J Transl Res, 2018, 10(7):2055-2067
S2727	Dacomitinib (PF299804, PF299) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay, effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Phase 2.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 J Thorac Oncol, 2019, 10.1016/j.jtho.2019.09.195 Clin Cancer Res, 2019, 25(2):641-651
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 Cell Biol, 2019, 21(8):1027-1040 Oncogene, 2019, 38(37):6399-6413 Clin Cancer Res, 2018, 24(13):3126-3136	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.	Gut, 2019, 68(6):1024-1033 Nat Commun, 2019, 10(1):2919 Cell Rep, 2019, 26(1):65-78
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 Res, 2019, 79(1):209-219 Int J Mol Sci, 2019, 20(13) Mol Pharmacol, 2019, 95(5):528-536	(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) 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.	Cell Death Dis, 2019, 10(3):191 Mol Cancer Res, 2019, 17(5):1195-1206 J Steroid Biochem Mol Biol, 2019, 187:58-67	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 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.	Oncotarget, 2016, 7(24):36168-36184 Oncogene, 2015, 10.1038/onc.2015.59 Int J Clin Exp Pathol, 2014, 7(11):7663-7671	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. Phase2.	Nat Cell Biol, 2019, 21(6):778-790 Korean J Parasitol, 2017, 55(5):491-503 Pathol Oncol Res, 2015, 10.1007/s12253-015-9916-9	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.	Asian J Androl, 2016, 10.4103/1008-682X Oncotarget, 2016, 7(24):36956-36970 Genes Cancer, 2014, 5(7-8):261-72	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.	Mol Pharmacol, 2019, 95(5):528-536 Oncogenesis, 2018, 7(1):5 Oncotarget, 2017, 8(14):22414-22432	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 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).	Transl Oncol, 2018, 11(6):1406-1418 Transl Lung Cancer Res, 2017, 6(5):600-610 Oncotarget, 2017, 8(58):98771-98781	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).		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).	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	AST-1306 AST-1306 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.	Cell Signal, 2020, 65:109439 Cell Rep, 2019, 28(9):2331-2344 Biochem Biophys Res Commun, 2018, 504(2):427-433	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, AVL-301) 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.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Nat Med, 2018, 24(5):638-646 Nat Commun, 2018, 9(1):4655	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 Genistein, 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.	Mol Cell, 2019, 75(6):1103-1116.e9 Cancer Manag Res, 2018, 10:6205-6216 Drug Deliv, 2018, 25(1):1258-1265
S2755	Varlitinib Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.	Pharmaceutics, 2018, 10(3) Oncol Rep, 2018, 40(2):635-646 Cancer Genet, 2017, 216-217:128-141
S2922	Icotinib Icotinib 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.	Mol Pharmacol, 2019, 95(5):528-536 Sci Signal, 2018, 11(549) Nat Chem Biol, 2016, 12(11):923-930
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.	Biol Open, 2018, 7(1) J Mol Med, 2018, 10.1007/s00109-018-1724-8 Oncol Rep, 2017, 37(1):66-76	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.	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.	Theranostics, 2017, 7(3):664-676	(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 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.	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 inhibits EGFR with IC50 of 35 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 (YH25448,GNS-1480) 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	AZD9291 Osimertinib (AZD9291) 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 Med, 2019, 25(1):111-118 Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Nat Commun, 2019, 10(1):2701	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) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.	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.
S8294	Olmutinib (HM61713, BI 1482694) Olmutinib 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
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.	Oncogene, 2019, 38(15):2690-2705 Onco Targets Ther, 2019, 12:6033-6043 Exp Ther Med, 2018, 15(5):4284-4290
S7786	Erlotinib Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.	Nat Med, 2019, 25(1):111-118 Cell, 2019, 178(4):807-819 Cancer Cell, 2019, 35(3):504-518	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.
S5098	Gefitinib hydrochloride Gefitinib is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively.	Br J Cancer, 2019, 120(3):306-316 Respir Res, 2019, 20(1-:270 Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0248-2
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.	Circulation, 2019, 139(22):2570-2584 Clin Cancer Res, 2018, 24(5):1227-1239 Cancer Discov, 2017, 7(6):575-585	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.	Clin Cancer Res, 2019, 25(8):2575-2587 Cancer Lett, 2019, 458:29-38 Drug Metab Dispos, 2019, 10.1124/dmd.118.084210
S7358	Poziotinib (HM781-36B) Poziotinib (HM781-36B) 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. Phase 2.	Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001 Nat Med, 2018, 24(5):638-646 Cancer Cell, 2018, 34(5):807-822
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 ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.	Cell Syst, 2019, 8(2):97-108 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104 Clin Cancer Res, 2018, 24(17):4162-4174	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 is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.	Arch Toxicol, 2019, 10.1007/s00204-019-02453-2 Respir Res, 2019, 20(1-:270 Thorac Cancer, 2019, 10(10):1868-1878
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.	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, NVS-816) 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 Nat Med, 2018, 24(5):638-646
S3759	Norcantharidin Norcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
S7926	Lifirafenib (BGB-283) Lifirafenib (BGB-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.	Cell Rep, 2019, 29(3):573-588 Oncotarget, 2019, 10(23):2237-2251
S4667	Lidocaine hydrochloride Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.
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.
S8242	EAI045 EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
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.
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.