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. Dual mTORC1/C2 inhibitor
SKU | RCLST031808 |
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CAS number | 1009298-09-2 |
Molecular Formula | C25H31N5O4 |
Catalog Number | RCLST031808 |
Chemical Name | AZD8055 |
Synonyms | 5-[2,4-Bis[(3S)-3-methyl-4-morpholinyl]pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol; [5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]- 2-methoxyphenyl]methanol; AZD 8055; [5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[5,6-e]py |
Molecular Weight | 465.54 |
Solubility | DMSO (Slightly), Methanol (Slightly, Sonicated) |
Stability | No Data Available |
Appearance | Pale Yellow to Light Yellow Solid |
Storage Condition | Refrigerator |