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[5-[2,4-二((3S)-3-甲基吗啉-4-基)吡啶并[2,3-d]嘧啶-7-基]-2-甲氧基苯基]甲醇
(5-(2,4-Bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol
化合物简介
A potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. 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. 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.
基本信息
CAS：1009298-09-2
中文别名：5-[2,4-双[(3S)-3-甲基-4-吗啉]吡啶并[2,3-d]嘧啶-7-基]-2-甲氧基苯甲醇;
英文别名：[5-[2,4-bis[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol;
分子式：C25H31N5O4
分子量：465.545
精确质量：465.238
Psa：93.07
Logp：2.7729
中文别名：5-[2,4-双[(3S)-3-甲基-4-吗啉]吡啶并[2,3-d]嘧啶-7-基]-2-甲氧基苯甲醇;
英文别名：[5-[2,4-bis[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol;
分子式：C25H31N5O4
分子量：465.545
精确质量：465.238
Psa：93.07
Logp：2.7729
编号系统
UNII：970JJ37FPW
物化性质
密度：1.248
沸点：694.302ºC at 760 mmHg
闪点：373.701ºC
沸点：694.302ºC at 760 mmHg
闪点：373.701ºC
安全信息
生产方法及用途
合成路线
上游原料
下游产品
图谱
13C NMR : Predict
1H NMR : Predict
