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EGFR/HER2 Epidermal growth factor receptor/Human epidermal growth factor receptor-2

Inhibitors

Cat.No.  Name Information
M3517 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.
M1802 Lapatinib Ditosylate Lapatinib Ditosylate (CAS 388082-78-8) is a selective and effective inhibitor of EGFR kinase (Ki = 3 nM), ErbB-2 kinase (Ki = 13 nM) and ErbB-4 kinase (Ki = 347 nM).
M1749 Gefitinib Gefitinib (ZD1839) is an EGFR tyrosine kinase and Akt phosphorylation inhibitor. Gefitinib significantly down-regulates CD47 expression and increases DC phagocytosis in non-small cell lung cancer cells such as PC9, H1437 and H1573. Gefitinib combined with CD47 antibody can enhance the phagocytosis of macrophages.
M5621 Erlotinib Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
M1913 Neratinib Neratinib (HKI-272) is an orally available, irreversible inhibitor of Her 2 tyrosine kinase.
M4850 PD153035 PD153035 is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM.
M4805 BIBX 1382 BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).
M4208 (-)-Epigallocatechin gallate (-)-Epigallocatechin Gallate is an antioxidant polyphenol flavonoid form green tea, and inhibits the activation of EGFR, HER2 and HER3, with antitumor activity.
M4002 Chrysophanic acid Chrysophanic acid, also known as chrysophanol, is a fungal isolate and a natural anthraquinone with anti-cancer activity.
M3780 XL647 XL647 is an extremely potent and selective inhibitor of EGFR phosphorylation (IC50 = 0.3 nM).
M3689 PD153035 hydrochloride PD153035 hydrochloride is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM.
M3684 Canertinib dihydrochloride Canertinib 2HCl 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.
M3569 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,
M3560 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.
M3553 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.
M3517 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.
M3491 OSI-420 OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
M3238 4-Quinazolinamine 4-Quinazolinamine (4-Aminoquinazoline) is a potent and highly selective EGFR tyrosine kinase inhibitor.
M3217 AV-412 AV-412 is a second-generation, orally bioavailable dual EGFR/HER2 tyrosine kinase inhibitor.
M3199 Varlitinib ARRY334543 is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively.
M3098 AG 879 Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
M2916 PD168393 PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.
M2464 BMS-690514 BMS-690514 is a potent inhibitor of EGFR and VEGFR2 with IC50 of 5 nM and 50 nM, respectively.
M2424 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, respectively.
M2312 AG-1478 AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM.



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