| 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. |
| M4749 | Cyasterone | Cyasterone, a natural EGFR inhibitor, was primarily isolated from Ajuga Decumbens Thunb (Labiatae). Cyasterone showed antiproliferative effects by inducing apoptosis and cell cycle arrest. Cyasterone could be used in studies against human tumors. |
| 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 (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). |
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