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Description

Category: Aromatics, Heterocycles, Pharmaceuticals, Intermediates and Fine Chemicals, Protein Kinase Inhibitors and Activators /// Appearance: Pale Yellow to Light Yellow Solid /// Application Notes: 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. /// 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)|