EGFR

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研究分野

阻害剤の選択性比較
溶解度

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
S9414	Cyasterone	-1 mg/mL	100 mg/mL	-1 mg/mL
S5078	Osimertinib mesylate	-1 mg/mL	9 mg/mL	-1 mg/mL
S8741	Avitinib (AC0010)	<1 mg/mL	97 mg/mL	97 mg/mL
S5098	Gefitinib hydrochloride	1 mg/mL	8 mg/mL	1 mg/mL
S2111	Lapatinib	<1 mg/mL	100 mg/mL	<1 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
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
S7206	CNX-2006	<1 mg/mL	100 mg/mL	29 mg/mL
S7298	AZ5104	<1 mg/mL	97 mg/mL	23 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
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
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
S8312	NSC228155	<1 mg/mL	15 mg/mL	<1 mg/mL

亜型選択性的な製品

EGFR製品

All (55) EGFR阻害剤(54) 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.	J Thorac Oncol, 2018, 13(6):810-820
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, 2012, 151(5):937-50 Nat Genet, 2012, 44(8):852-60 Cancer Discov, 2013, 3(12):1404-15	Erlotinib IC50 in HCC827 cell lines measured 48h after treatment with vehicle (control) or with erlotinib. Erlotinib IC50 is shown in parentheses. Data are representative of 3 independent experiments. Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers.
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.	Nature, 2017, 547(7664):453-457 Nature, 2016, 534(7609):647-51 Nature, 2012, 483(7387):100-3	c, HCC4006 lung cancer cells that have acquired a high-mesenchymal state concomitant with becoming resistant to gefitinib (red curve) exhibit increased sensitivity to GPX4 inhibition.
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.	Cancer Cell, 2012, 21(4):488-503 Gut, 2015, 10.1136/gutjnl-2014-309026 Sci Transl Med, 2015, 7(284):284ra57	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, 2016, 534(7609):647-51 Cancer Discov, 2015, 5(7):713-22 Cancer Discov, 2013, 3(2):168-81	Immunoblot analysis of serum starved H2030 cells pre-treated with 500 nM or 1 µM of gefitinib, crizotinib, CP-724714, or afatinib for 12 hr, followed by stimulation with EGF, HGF, NRG1, or their combination (50 ng/ml) for 10 min.
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.	Cancer Discov, 2012, 2(5):458-71 Cancer Lett, 2014, 344(1):90-100 J Exp Clin Cancer Res, 2018, 37(1):80
S8584^新	Theliatinib (HMPL-309)
S9414^新	Cyasterone Cyasterone is the main phytoecdysteroid component found in Cyathula capitata. It is a natural EGFR inhibitor and maybe a promising anti-cancer agent.
S5078^新	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.
S8741^新	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.
S5098^新	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.
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.	Nature, 2016, 538(7626):477-482 Cancer Cell, 2015, 27(3):397-408 Cancer Cell, 2012, 21(4):488-503	Sensitivity to the ErbB1/ErbB2 inhibitor lapatinib is highest for cancer cells from late-stage tumors in culture (mean ± SEM, p = 0.04 or 0.02 as indicated, Student’s t test; values represent the averages of four experiments, each done in triplicate with primary cells from independent mice).
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.	Cancer Res, 2014, 74(1):341-52 Cell Death Dis, 2014, 5:e1194 J Biol Chem, 2016, 291(16):8453-64	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CP-724714 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
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.	Gut, 2015, 10.1136/gutjnl-2014-309026 J Thorac Oncol, 2018, 13(5):727-731 Clin Cancer Res, 2015, 21(23):5305-13
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 Commun, 2015, 6:6377 Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560 Clin Cancer Res, 2012, 18(6):1663-71	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, 2015, 10.1136/gutjnl-2014-309026 Clin Cancer Res, 2014, 20(17):4559-73 Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2701	Western blot analysis confirm suppression of the biomarker p-EGFR upon treatment with EGFR TKIs in U-CH1 and UM-Chor1. Cells were serum-starved overnight before they were treated with a range of concentrations of the EGFR inhibitors for 4 h and then EGF-spiked (50 ng/ml) for 15 min. Endogenous controls (non-serum-starved, non-EGF-spiked), untreated controls (serum-starved, non-EGF-spiked) and vehicle controls (serum-starved, treated with 2.5% DMSO, EGF-spiked) were included. Phospho-EGFR was measured by western blot.
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.	J Chem Inf Model, 2014, 54(3):881-93 ACS Med Chem Lett, 2013, 4(9):858-62 Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066	(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 Rep, 2013, 4(4):764-75 Pharmacol Res, 2017, 119:72-88 J Pharmacol Exp Ther, 2012, 341(2):386-95	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.	Oncogene, 2015, 10.1038/onc.2015.59 J Immunol, 2012, 188(9):4581-9 Antivir Res, 2011, 89(1):64-70	B. Increased of cell migration induced by EGF is inhibited by a selective ATP competitive inhibitor of EGFR (PD153035). Histograms showing HCT-116 cell migration with or without treatment by EGF +/− PD153035. Results are expressed as mean ± SEM. ***p<0.001, sample significantly different from control (N=3, n=7, Kruskal-Wallis test).
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.	Cancer Cell, 2012, 22(5):656-67 J Cell Mol Med, 2013, 17(5):648-56 Asian J Androl, 2016, 10.4103/1008-682X	RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT.
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.	Prostate, 2013, 73(13):1453-61 PLoS One, 2015, 10(4):e0123623 Int J Clin Exp Pathol, 2013, 6(10):2082-91	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).	Carcinogenesis, 2010, 31(11), 1948-1955 Int J Clin Exp Pathol, 2013, 6(10):2082-91 Korean J Parasitol, 2016, 54(1):31-8	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).		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.	Cancer Lett, 2014, 350(1-2):61-8 Oncol Rep, 2015, 32(6):2511-6 Oncol Rep, 2014, 32(6):2511-6	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 Discov, 2015, 5(7):713-22 J Thorac Oncol, 2015, 10.1097/JTO.0000000000000500 Clin Cancer Res, 2015, 21(23):5305-13	Immunohistochemical studies reveal the tumor cells to be negative for chromogranin and synaptophysin pre-rociletinib and positive for both neuroendocrine markers in the post-rociletinib liver biopsy. The results, in conjunction with the morphology, are consistent with the diagnosis of small cell carcinoma in the rociletinib-resistant specimen. H&E, hematoxylin and eosin.
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.	J Electroanal Chem, 2015, 742:54–61 Drug Deliv, 2018, 25(1):1258-1265 Cell Physiol Biochem, 2018, 51(6):2564-2574
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.	J Cell Biochem, 2014, 115(8):1381-91 Pharmaceutics, 2018, 10(3) Oncol Rep, 2017, 37(1):66-76
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).	Oral Oncology, 2016, 10.1016/j.oraloncology.2016.05.010 Oncogene, 2017, 36(45):6235-6243 Oncotarget, 2015, 5(12):4529-42	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.
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.	Oncol Rep, 2017, 37(1):66-76 Biol Open, 2018, 7(1) J Mol Med, 2018, 10.1007/s00109-018-1724-8	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.	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.
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.
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.
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.	Cancer Discov, 2015, 5(11):1155-63 Cancer Discov, 2015, 5(7):713-22 J Thorac Oncol, 2018, 13(7):915-925	(C,D) The Ba/F3 cells expressing EGFR-T854A/C797S/del19 (C) and EGFR-T854A/C797S/L858R (D) were treated with gefitinib, afatinib, osimertinib, and brigatinib for 6 hours at indicated concentrations. EGFR phosphorylation and downstream signal pathway were evaluated by Western blotting.
S7557	CL-387785 (EKI-785) CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.	Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2789 Nature, 2017, 550(7675):270-274	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.
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.	J Nutr Biochem, 2013, 24(11):1953-62 J Cell Mol Med, 2017, 10.1111/jcmm.13169 PLoS One, 2013, 8(8): e69519	(a) Huh7 cells were incubated with HCVcc of JFH-1 for 2 h before overlaying with 1% agarose dissolved in culture medium or with AR3A anti-E2 neutralizing antibodies, in the presence of 20 μg/ml SZA. EGCG (50 μM) was introduced as a positive control. At 48 h post-infection, infected cells were quantified by IF. Nuclei were stained with DAPI. (b) Numbers of cells per positive colony were determined in 15 foci.
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.	Cell, 2012, 151(5):937-50 Nat Genet, 2012, 44(8):852-60 Cancer Discov, 2015, 5(11):1155-63	Erlotinib IC50 in HCC827 cell lines measured 48h after treatment with vehicle (control) or with erlotinib. Erlotinib IC50 is shown in parentheses. Data are representative of 3 independent experiments. Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers.
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.	Cancer Discov, 2017, 7(6):575-585 Cancer Discov, 2013, 3(2):168-81 Gut, 2015, 10.1136/gutjnl-2014-309026	(F) Stably transduced MCF10A cells were treated with the indicated drugs at 100 nM for 4 h in EGF- and serum-free media. Cell lysates were subjected to immunoblot analyses with the indicated antibodies.
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.	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.
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.	Clin Cancer Res, 2018, 24(17):4162-4174 Cancer Sci, 2018, 109(10):3149-3158 Sci Rep, 2016, 6:26125	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.
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.		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.
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.
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.
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.	J Thorac Oncol, 2018, 13(6):810-820
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, 2012, 151(5):937-50 Nat Genet, 2012, 44(8):852-60 Cancer Discov, 2013, 3(12):1404-15	Erlotinib IC50 in HCC827 cell lines measured 48h after treatment with vehicle (control) or with erlotinib. Erlotinib IC50 is shown in parentheses. Data are representative of 3 independent experiments. Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers.
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.	Nature, 2017, 547(7664):453-457 Nature, 2016, 534(7609):647-51 Nature, 2012, 483(7387):100-3	c, HCC4006 lung cancer cells that have acquired a high-mesenchymal state concomitant with becoming resistant to gefitinib (red curve) exhibit increased sensitivity to GPX4 inhibition.
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.	Cancer Cell, 2012, 21(4):488-503 Gut, 2015, 10.1136/gutjnl-2014-309026 Sci Transl Med, 2015, 7(284):284ra57	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, 2016, 534(7609):647-51 Cancer Discov, 2015, 5(7):713-22 Cancer Discov, 2013, 3(2):168-81	Immunoblot analysis of serum starved H2030 cells pre-treated with 500 nM or 1 µM of gefitinib, crizotinib, CP-724714, or afatinib for 12 hr, followed by stimulation with EGF, HGF, NRG1, or their combination (50 ng/ml) for 10 min.
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.	Cancer Discov, 2012, 2(5):458-71 Cancer Lett, 2014, 344(1):90-100 J Exp Clin Cancer Res, 2018, 37(1):80
S8584^新	Theliatinib (HMPL-309)
S9414^新	Cyasterone Cyasterone is the main phytoecdysteroid component found in Cyathula capitata. It is a natural EGFR inhibitor and maybe a promising anti-cancer agent.
S5078^新	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.
S8741^新	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.
S5098^新	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.
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.	Nature, 2016, 538(7626):477-482 Cancer Cell, 2015, 27(3):397-408 Cancer Cell, 2012, 21(4):488-503	Sensitivity to the ErbB1/ErbB2 inhibitor lapatinib is highest for cancer cells from late-stage tumors in culture (mean ± SEM, p = 0.04 or 0.02 as indicated, Student’s t test; values represent the averages of four experiments, each done in triplicate with primary cells from independent mice).
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.	Cancer Res, 2014, 74(1):341-52 Cell Death Dis, 2014, 5:e1194 J Biol Chem, 2016, 291(16):8453-64	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CP-724714 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
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.	Gut, 2015, 10.1136/gutjnl-2014-309026 J Thorac Oncol, 2018, 13(5):727-731 Clin Cancer Res, 2015, 21(23):5305-13
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 Commun, 2015, 6:6377 Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560 Clin Cancer Res, 2012, 18(6):1663-71	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, 2015, 10.1136/gutjnl-2014-309026 Clin Cancer Res, 2014, 20(17):4559-73 Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2701	Western blot analysis confirm suppression of the biomarker p-EGFR upon treatment with EGFR TKIs in U-CH1 and UM-Chor1. Cells were serum-starved overnight before they were treated with a range of concentrations of the EGFR inhibitors for 4 h and then EGF-spiked (50 ng/ml) for 15 min. Endogenous controls (non-serum-starved, non-EGF-spiked), untreated controls (serum-starved, non-EGF-spiked) and vehicle controls (serum-starved, treated with 2.5% DMSO, EGF-spiked) were included. Phospho-EGFR was measured by western blot.
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.	J Chem Inf Model, 2014, 54(3):881-93 ACS Med Chem Lett, 2013, 4(9):858-62 Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066	(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 Rep, 2013, 4(4):764-75 Pharmacol Res, 2017, 119:72-88 J Pharmacol Exp Ther, 2012, 341(2):386-95	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.	Oncogene, 2015, 10.1038/onc.2015.59 J Immunol, 2012, 188(9):4581-9 Antivir Res, 2011, 89(1):64-70	B. Increased of cell migration induced by EGF is inhibited by a selective ATP competitive inhibitor of EGFR (PD153035). Histograms showing HCT-116 cell migration with or without treatment by EGF +/− PD153035. Results are expressed as mean ± SEM. ***p<0.001, sample significantly different from control (N=3, n=7, Kruskal-Wallis test).
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.	Cancer Cell, 2012, 22(5):656-67 J Cell Mol Med, 2013, 17(5):648-56 Asian J Androl, 2016, 10.4103/1008-682X	RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT.
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.	Prostate, 2013, 73(13):1453-61 PLoS One, 2015, 10(4):e0123623 Int J Clin Exp Pathol, 2013, 6(10):2082-91	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).	Carcinogenesis, 2010, 31(11), 1948-1955 Int J Clin Exp Pathol, 2013, 6(10):2082-91 Korean J Parasitol, 2016, 54(1):31-8	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).		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.	Cancer Lett, 2014, 350(1-2):61-8 Oncol Rep, 2015, 32(6):2511-6 Oncol Rep, 2014, 32(6):2511-6	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 Discov, 2015, 5(7):713-22 J Thorac Oncol, 2015, 10.1097/JTO.0000000000000500 Clin Cancer Res, 2015, 21(23):5305-13	Immunohistochemical studies reveal the tumor cells to be negative for chromogranin and synaptophysin pre-rociletinib and positive for both neuroendocrine markers in the post-rociletinib liver biopsy. The results, in conjunction with the morphology, are consistent with the diagnosis of small cell carcinoma in the rociletinib-resistant specimen. H&E, hematoxylin and eosin.
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.	J Electroanal Chem, 2015, 742:54–61 Drug Deliv, 2018, 25(1):1258-1265 Cell Physiol Biochem, 2018, 51(6):2564-2574
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.	J Cell Biochem, 2014, 115(8):1381-91 Pharmaceutics, 2018, 10(3) Oncol Rep, 2017, 37(1):66-76
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).	Oral Oncology, 2016, 10.1016/j.oraloncology.2016.05.010 Oncogene, 2017, 36(45):6235-6243 Oncotarget, 2015, 5(12):4529-42	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.
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.	Oncol Rep, 2017, 37(1):66-76 Biol Open, 2018, 7(1) J Mol Med, 2018, 10.1007/s00109-018-1724-8	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.	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.
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.
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.
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.	Cancer Discov, 2015, 5(11):1155-63 Cancer Discov, 2015, 5(7):713-22 J Thorac Oncol, 2018, 13(7):915-925	(C,D) The Ba/F3 cells expressing EGFR-T854A/C797S/del19 (C) and EGFR-T854A/C797S/L858R (D) were treated with gefitinib, afatinib, osimertinib, and brigatinib for 6 hours at indicated concentrations. EGFR phosphorylation and downstream signal pathway were evaluated by Western blotting.
S7557	CL-387785 (EKI-785) CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.	Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2789 Nature, 2017, 550(7675):270-274	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.
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.	J Nutr Biochem, 2013, 24(11):1953-62 J Cell Mol Med, 2017, 10.1111/jcmm.13169 PLoS One, 2013, 8(8): e69519	(a) Huh7 cells were incubated with HCVcc of JFH-1 for 2 h before overlaying with 1% agarose dissolved in culture medium or with AR3A anti-E2 neutralizing antibodies, in the presence of 20 μg/ml SZA. EGCG (50 μM) was introduced as a positive control. At 48 h post-infection, infected cells were quantified by IF. Nuclei were stained with DAPI. (b) Numbers of cells per positive colony were determined in 15 foci.
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.	Cell, 2012, 151(5):937-50 Nat Genet, 2012, 44(8):852-60 Cancer Discov, 2015, 5(11):1155-63	Erlotinib IC50 in HCC827 cell lines measured 48h after treatment with vehicle (control) or with erlotinib. Erlotinib IC50 is shown in parentheses. Data are representative of 3 independent experiments. Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers.
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.	Cancer Discov, 2017, 7(6):575-585 Cancer Discov, 2013, 3(2):168-81 Gut, 2015, 10.1136/gutjnl-2014-309026	(F) Stably transduced MCF10A cells were treated with the indicated drugs at 100 nM for 4 h in EGF- and serum-free media. Cell lysates were subjected to immunoblot analyses with the indicated antibodies.
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.	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.
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.	Clin Cancer Res, 2018, 24(17):4162-4174 Cancer Sci, 2018, 109(10):3149-3158 Sci Rep, 2016, 6:26125	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.
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.		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.
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.
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.