应用 |
A potent and selective inhibitor of EGFR phosphorylation. |
产品介绍 |
AST-1306 TsOH是一种新型,不可逆的EGFR和ErbB2抑制剂,IC50分别为0.5 nM和3 nM,对突变型EGFR T790M/L858R也有效,作用于过表达ErbB2的细胞更有效,作用于ErbB家族比作用于其他激酶选择性高3000倍。 |
备注 |
AST-1306 TsOH 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, |
生化机理 |
AST-1306 TsOH is a potent(pM) and selective inhibitor of EGFR and ErbB4 (IC50 = 500pM and 800 pM, respectively). AST 1306 blocks phosphorylation of EGFR and also prevents downstream pathways. AST 1306 also dose-dependently inhibits EGF-induced EGFR phosphorylation in the A549 cancer cell line. |
别名 |
N-[4-[[3-氯-4-[(3-氟苯基)甲氧基]苯基]氨基]-6-喹唑啉基]-2-丙烯酰胺对甲苯磺酸盐;N-[4-[[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-2-propenamide 4-methylbenzenesulfonate;AST-1306 (p-Toluenesulfonic acid); AST1306 (p-Toluenesulfonic acid); AST 1306 (p-Toluenesulfonic acid;AST-6 |