别名:酪氨酸激酶抑制剂AG 1478; N-(3-氯苯基)-6,7-二甲氧基-4-氨基喹唑啉;(3-氯苯基)(6,7-二甲氧基喹唑啉-4-基)胺 ;Tyrphostin AG-1478;AG 1478;NSC 693255;AG1478;N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinamine;3-chlorophenyl)(6,7-dimethoxyquinazolin-4-yl)amine

溶解性	25°C: DMSO 25 mg/mL; Water <1 mg/mL; Ethanol 13 mg/mL
存贮条件	储存温度-20°C
密度	1.3370
荧光	否
IC50	否
pK Values	否

产品介绍

AG-1478 (NSC 693255)是高效EGFR选择性抑制剂，IC50为3 nM，对HER2-Neu，PDGFR，Trk，Bcr-Abl和InsR无活性。

生化机理

AG1478 inhibited EGFR phosphorylation in CNE2 cells without reduced expression of EGFR protein. The activation of Akt and MAPK which are downstream molecules of EGFR signaling pathway, were also inhibited by AG1478 . Although AG 1478 inhibited cell growth, DNA synthesis, EGFR tyrosine kinase activity, and receptor autophosphorylation of each cell line in a dose-dependent manner, it was significantly more potent in U87MG. delta EGFR cells than in the other two cell lines . in vivo: At the lowest dose, plasma drug levels after the cessation of infusion declined with a half-life of approximately 43 min. EGFR activity, measured both by autophosphorylation and downstream signalling, was inhibited in a dose-dependent manner by injection of AG1478 in mice bearing xenografts of the human glioblastoma cell line U87MG