A potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8nM. 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. 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 No: 1009298-09-2 Molecular Formula: C25H31N5O4 Molecular Weight: 465.54 Elemental Analysis: Calculated: 64.50% C, 6.71% H, 15.04% N Found: As reported Appearance: Supplied as a pale yellow to light yellow solid Purity: 95% Melting Point: 204-207C Solubility: DMSO (slightly), Methanol (slightly) Method for Determining Identity: Proton NMR (CD3OD, DMSO-d6) and MS TLC Conditions: SiO2, Dichloromethane : Methanol (9 : 1). Visualized with AMCS, KMnO4 and naked eye (single spot, Rf = 0.65). Storage and Stability: Store at -4C. Stable for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Caution: Hygroscopic. Store under inert atmosphere.
Molecular Weight:
465.54
CAS Number:
[1009298-09-2]
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