N-[2-[(3,5-二甲氧基苯基)氨基]喹喔啉-3-基]-4-[(4-甲基-3-甲氧基苯基)羰基]氨基苯磺酰胺

溶解度:Soluble in DMSO

储存条件:at -20℃ 2 years

生物活性

AZD8055,Potent and selective mTOR inhibitor, with IC50 values to be 0.8 nM and selectivity ca 1000-fold against class I PI3K and other PIKKs.In vitro, AZD8055 potently inhibits proliferation and induces autophagy in H838 and A549 cells.In vivo, AZD8055 induces a dose-dependent pharmacodynamic effect on phosphorylated S6 and phosphorylated AKT at plasma concentrations leading to tumor growth inhibition. It inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 were fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation.

参考文献

CM Chresta et al. AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity. Cancer Res. 2010, 70(1), 288-298.