Product Categories

EGFR Inhibitors

EGFR Inhibitors (33)
water-soluble

Cat.No.	Product Name	Information	Product Citations
S1023	Erlotinib HCl	Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM.	Nat Genet, 2012, 44(8):852-60 Cell, 2012, 151(5):937-50 J Clin Invest, 2012, 122(9):3197-210
S1025	Gefitinib (Iressa)	Gefitinib (Iressa, 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, 2012, 483(7387), 100-103 Cell, 2012, 151(5):937-50 Mol Syst Biol, 2011, 7, 486
S1011	Afatinib (BIBW2992)	BIBW2992 (Afatinib, Tomtovok, Tovok) 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.	Clin Cancer Res, 2012, 18(6), 1663-1671 Eur J Cancer, 2012, ahead of print Int J Proteomics, 2011, 2011, 215496
S1143	AG-490	AG-490 (Tyrphostin B42) is an inhibitor of EGFR, ErbB2 and JAK2 with IC50 of 0.1 μM, 13.5 μM, and ~10 μM, respectively.	Prostate, 2012, ahead of print Biochem Biophys Res Commun, 2013, 429(3-4), 156-162
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, respectively.	Cancer Cell, 2012, 21(4):488-503 ACS Nano, 2012, 6(10), 8525-8535 Mol Oncol, 2012, ahead of print
S4911	BMS-690514	BMS-690514 is a novel pan-HER/VEGFR inhibitor.
S1028	Lapatinib Ditosylate (Tykerb)	Lapatinib Ditosylate (GW572016, GW2016, Tykerb, Tyverb) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.	Proc Natl Acad Sci U S A, 2012, 109(17), 6584-6589 Oncogene, 2012, ahead of print Carcinogenesis, 2010, 31(11), 1948-1955
S1167	CP-724714	CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM and also inhibits EGFR with IC50 of 6.4 μM.
S8009	AG 18 (Tyrphostin 23)	AG 18 inhibits EGFR with IC50 of 35 μM.
S2867	WHI-P154	WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM and also inhibits EGFR with IC50 of 4 nM.
S2784	TAK-285	TAK-285 is a novel dual HER2 and EGFR inhibitor with IC50 of 17 nM and 23 nM, respectively.
S2185	AST-1306	AST-1306 is a novel irreversible inhibitor of EGFR and ErbB4 with IC50 of 0.5 nM and 0.8 nM, respectively.
S2755	ARRY334543	ARRY334543 is a selective and potent ErbB1 and ErbB2 inhibitor with IC50 of 7 nM and 2 nM, respectively.
S2752	Arry-380	ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM and also inhibits EGFR with IC50 of 4 μM.
S2922	Icotinib	Icotinib is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with IC50 of 5 nM.
S2728	AG-1478 (Tyrphostin AG-1478)	AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM.	J Pharmacol Exp Ther, 2012, 341(2):386-95 J Chromatogr B Analyt Technol Biomed Life Sci, 2011, 879(32), 3812-3817 A dissertation submitted to the faculty of the graduate school of the university of minnesota, ,
S2895	Tyrphostin 9 (SF 6847)	SF 6847 is an inhibitor of EGFR with IC50 of 460 μM.
S2727	Dacomitinib (PF299804,PF-00299804)	PF299804 is a potent, irreversible pan-ErbB inhibitor against ErbB1, ErbB2 and ErbB4 with IC50 of 6 nM, 45.7 nM and 73.7 nM, respectively.
S2733	AV-412	AV-412 is a second-generation, orally bioavailable dual EGFR/HER2 tyrosine kinase inhibitor.
S2826	Desmethyl Erlotinib (CP-473420)	Desmethyl Erlotinib (CP-473420) is a free base of OSI-420, which is an active metabolite of Erlotinib which is an orally active EGFR inhibitor for human EGFR with IC50 of 2 nM.
S2205	OSI-420	OSI-420 is an active metabolite of Erlotinib which is an orally active EGFR inhibitor for inhibition of human EGFR and EGFR autophosphorylation with IC50 of 2 nM and 20 nM, respectively.	Submitted in partial fulfillment of the requirements, , Carcinogenesis, 2010, 31(11), 1948-1955 Sci Pharm, 2012, 80(3):633-46
S2192	AZD8931	AZD8931 is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM, respectively.
S2150	Neratinib (HKI-272)	Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM, respectively.	Cancer Discov, 2012, 2(5):458-71 Cancer Discov, 2012, ahead of print Cancer Discov, 2013, 3(2):224-37
S1486	AEE788 (NVP-AEE788)	AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM and also inhibits VEGFR2 and Flt with IC50 of 77 nM and 59 nM, respectively.
S1392	Pelitinib (EKB-569)	Pelitinib (EKB-569) is a potent EGFR inhibitor with IC50 of 38.5 nM.	J Immunol, 2012, 188(9):4581-9
S1194	CUDC-101	CUDC-101 is a potent multi-target inhibitor targeting HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, respectively.
S1179	WZ8040	WZ8040 is a novel mutant-selective irreversible EGFR^T790M inhibitor.
S1173	WZ4002	WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR^L858R and EGFR^L858R/T790M with IC50 of 2 nM and 8 nM, respectively.	Clin Cancer Res, 2012, 18(6), 1663-1671 Mol Cancer Ther, 2012, 11(10):2149-57 PLoS One, 2012, 7(9):e42441
S1170	WZ3146	WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM, respectively.
S1083	XL647	XL647 is a novel spectrum-selective kinase inhibitor for EGFR, ErbB2, KDR, Flt-4 and EphB4 with IC50 of 0.3 nM, 16 nM, 1.5 nM, 8.7 nM and 1.4 nM, respectively.
S1079	PD153035 HCl	PD153035 is a potent and specific inhibitor of EGFR with K_i and IC50 of 5.2 pM and 29 pM, respectively.	Antivir Res, 2010, 89(1), 64-70
S1056	BMS-599626 (AC480)	BMS-599626 (AC480) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, respectively.	Cancer Cell, 2012, 22(5):656-67 Cancer Res, 2012, 72(12):3069-79
S1019	CI-1033 (Canertinib)	CI-1033 is a potent inhibitor of EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.	J Cell Sci, 2010, 123(Pt 18), 3102-3111 Carcinogenesis, 2010, 31(11), 1948-1955 Cell Cycle, 2009, 8(13), 2050-6

Inhibitory Selectivity
Solubility

Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1023	Erlotinib HCl	<1 mg/mL	3 mg/mL	<1 mg/mL
S1025	Gefitinib (Iressa)	<1 mg/mL	89 mg/mL	4 mg/mL
S1011	Afatinib (BIBW2992)	<1 mg/mL	97 mg/mL	15 mg/mL
S1143	AG-490	<1 mg/mL	59 mg/mL	6 mg/mL
S2111	Lapatinib	<1 mg/mL	100 mg/mL	<1 mg/mL
S1028	Lapatinib Ditosylate (Tykerb)	<1 mg/mL	185 mg/mL	<1 mg/mL
S1167	CP-724714	<1 mg/mL	94 mg/mL	94 mg/mL
S8009	AG 18 (Tyrphostin 23)	<1 mg/mL	37 mg/mL	37 mg/mL
S2867	WHI-P154	<1 mg/mL	75 mg/mL	<1 mg/mL
S2784	TAK-285	<1 mg/mL	110 mg/mL	54 mg/mL
S2185	AST-1306	<1 mg/mL	124 mg/mL	<1 mg/mL
S2755	ARRY334543	<1 mg/mL	6 mg/mL	<1 mg/mL
S2752	Arry-380	<1 mg/mL	114 mg/mL	<1 mg/mL
S2922	Icotinib	<1 mg/mL	78 mg/mL	7 mg/mL
S2728	AG-1478 (Tyrphostin AG-1478)	<1 mg/mL	25 mg/mL	13 mg/mL
S2895	Tyrphostin 9 (SF 6847)	<1 mg/mL	56 mg/mL	56 mg/mL
S2727	Dacomitinib (PF299804,PF-00299804)	<1 mg/mL	19 mg/mL	<1 mg/mL
S2826	Desmethyl Erlotinib (CP-473420)	<1 mg/mL	11 mg/mL	5 mg/mL
S2205	OSI-420	2 mg/mL	83 mg/mL	<1 mg/mL
S2192	AZD8931	<1 mg/mL	40 mg/mL	<1 mg/mL
S2150	Neratinib (HKI-272)	<1 mg/mL	2 mg/mL	<1 mg/mL
S1486	AEE788 (NVP-AEE788)	<1 mg/mL	88 mg/mL	<1 mg/mL
S1392	Pelitinib (EKB-569)	<1 mg/mL	13 mg/mL	<1 mg/mL
S1194	CUDC-101	<1 mg/mL	20 mg/mL	<1 mg/mL
S1179	WZ8040	<1 mg/mL	96 mg/mL	3 mg/mL
S1173	WZ4002	<1 mg/mL	13 mg/mL	<1 mg/mL
S1170	WZ3146	<1 mg/mL	93 mg/mL	<1 mg/mL
S1079	PD153035 HCl	<1 mg/mL	0.5 mg/mL	<1 mg/mL
S1056	BMS-599626 (AC480)	<1 mg/mL	113 mg/mL	20 mg/mL
S1019	CI-1033 (Canertinib)	<1 mg/mL	2 mg/mL	9 mg/mL

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EGFR Inhibitors

EGFR Inhibitors (33)water-soluble

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EGFR Inhibitors (33)
water-soluble