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製品情報 - Reference Compounds
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AZD 8055
| カタログ : |
C13352 |
| 製品の名前: |
AZD 8055 |
| 同義語: |
AZD-8055; AZD8055; AZD 8055 |
| 化学の名前: |
5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol |
| CASナンバー : |
1009298-09-2 |
| 構成 : |
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| 分子式: |
C25H31N5O4 |
| 分子量: |
465.54 |
| 純度: |
>98% |
| 使い方: |
AZD8055 is a novel ATP-competitive inhibitor of mTOR kinase activity with an IC50 of 0.8 nmol/L. AZD8055 showed excellent selectivity (~1,000-fold) against all class I phosphatidylinositol 3-kinase (PI3K) isoforms and other members of the PI3K-like kinase family. Furthermore, there was no significant activity against a panel of 260 kinases at concentrations up to 10 μmol/L. AZD8055 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. Notably, AZD8055 results in significant growth inhibition and/or regression in xenografts, representing a broad range of human tumor types. AZD8055 is currently in phase I clinical trials. |
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