| 应用 |
A potent and selective inhibitor of EGFR and ERBB phosphorylation. |
| 产品介绍 |
Dacomitinib (PF299804, PF299)是一种有效的，不可逆的pan-ErbB抑制剂，最有效作用于EGFR，IC50为6 nM，高效作用于携带EGFR或ERBB2突变型(抗Gefitinib)和携带EGFR T790M突变型的NSCLCs。 |
| 备注 |
PF-299804 is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM, effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Phase 2. |
| 生化机理 |
Dacomitinib is a potent inhibitor of EGFR T710M and is also an inhibitor of ERBB2 and ERBB4, although at approximately 10x the concentration necessary to inhibit phosphorylation of EGFR T710M (IC50 = 6nM, 45.7nM and 73.7nM, respectively). |
| 别名 |
达克替尼;(2E)-N-[4-[(3-氯-4-氟苯基)氨基]-7-甲氧基-6-喹唑啉基]-4-(1-哌啶基)-2-丁烯酰胺;PF299804;PF299PF-00299804;PF-299804;PF 299804;PF 00299804;(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide |
