| 应用 |
A potent and selective inhibitor of EGFR and HER2 |
| 产品介绍 |
Neratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂，IC50分别为59 nM和92 nM；微弱抑制KDR和Src，对Akt，CDK1/2/4， IKK-2， MK-2， PDK1， c-Raf和c-Met没有显著的抑制作用。Phase 3。 |
| 备注 |
Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3. |
| 生化机理 |
Neratinib is a potent and selective inhibitor of EGFR and Neu(HER2) (IC50 = 92 nM and 59 nM, respectively) by preventing phosphorylation of these proteins by their respective kinases. Neratinib displays activity against a variety of cancer cell lines, including A431, 3T3, and MDA-MB-435. Neratinib is an inhibitor of c-Src and Flk-1. |
| 别名 |
来那替尼; (2E)-N-[4-[[3-氯-4-[(吡啶-2-基)甲氧基]苯基]氨基]-3-氰基-7-乙氧基喹啉-6-基]-4-(二甲基氨基)丁-2-烯酰胺;HKI-272;HKI272;HKI 272;(2E)-N-[4-[[3-chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
