CAS:1009298-09-2|AZD8055

Catalogue Number:A808130
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]pyrimidin-7-yl]-2-methoxyphenyl]methanol
CAS Number:1009298-09-2
Molecular Formula:C₂₅H₃₁N₅O₄
Appearance:Pale Yellow to Light Yellow Solid
Melting Point:204 – 207°C
Molecular Weight:465.54
Storage:4°C
Solubility:DMSO (Slightly), Methanol (Slightly)
Category:Standards; Enzyme Activators and Inhibitors; Pharmaceutical/API Drug Impurities/Metabolites;
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);
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