85-2006-59　AZD8055 100mg　CAS No:1009298-09-2　162713

特徴

• 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
• Molecular Formula:C25H31N5O4
• Molecular Weight:465.54
• Elemental Analysis:Calculated: 64.50% C; 6.71% H; 15.04% NFound: As reported
• Appearance:Supplied as a pale yellow to light yellow solid
• Purity:≥95%
• Melting Point:204-207°C
• 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 -4°C. 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.