CAS 1009298-09-2: 5-[2,4-Bis[(3S)-3-methyl-4-morpholinyl]pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol

AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.

AZD-8055

Applications 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 References Chresta, C.M. et al.: Cancer Res., 70, 288 (2010); Sini, P. et al. Autophagy., 6 (2010); Marshall, G. et al.: Biochem. Soc. Trans., 39, 456 (2011);

Azd-8055

A selective and ATP-competitive inhibitor of mTOR kinase with an IC50 value of 0.8 nM. Inhibits growth of a range of tumor types in vivo and in vitro. Effective in preventing and treating endocrine-resistant breast cancer. Causes autophagy in H838 and A549 cells.