| Cat.No. | Name | Information |
|---|---|---|
| M3517 | Lapatinib | Lapatinib (GW572016) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively. |
| M1802 | Lapatinib ditosylate monohydrate | Lapatinib (GW572016) ditosylate monohydrate 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 (CP-358774) | Erlotinib (CP-358774) 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. |
| M1850 | WZ4002 | WZ4002 is a novel, selective EGFR kinase inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) with IC50 of 8 nM. |
| M1869 | Dacomitinib | Dacomitinib (PF-00299804) is an oral, irreversible, small molecule inhibitor of human epidermal growth factor receptor-1, -2, and -4 tyrosine kinases. |
| M5307 | Afatinib 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. |
| M2424 | AZD9291 (Osimertinib) | Osimertinib (AZD-9291) 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. |
| M1677 | Afatinib | Afatinib (BIBW 2992) is a novel irreversible dual EGFR and HER2 tyrosine kinase inhibitor. |
| 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 (TsOH) | 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 analog | ARRY-380 analog 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. |
| 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. |
| M2212 | Rociletinib (CO-1686) | Rociletinib (CO-1686) is a potent, novel inhibitor of EGFR L858R/T790M kinase with Ki of 21.5 nM and 303.3 nM, respectively. |
| M2117 | CNX-2006 | CNX-2006 is a novel irreversible EGFR inhibitor with IC50 value of <20 nM. |
| M2021 | AG 18 | AG-18 (Tyrphostin A23, tyrA23) inhibits EGFR with an IC50 of 35 μM. TyrA23 is also an inhibitor of CME and inhibits transferrin receptor internalization. |
| M1943 | Canertinib | Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). |
| M1919 | Mubritinib | Mubritinib (TAK-165) is a new potent inhibitor of human epidermal growth factor receptor 2 (HER2) tyrosine kinase (IC50 = 6 nM). |
| M1904 | Pelitinib | Pelitinib (EKB-569) is an irreversible EGFR tyrosine kinase inhibitor with IC50 of 38.5 nM. |
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