Description
AZD8055 can inhibit mTOR with IC50 of 0.8 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C25H31N5O4
Chemical Name
(5-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol
Solubility
DMSO 93 mg/mL Water 2 mg/mL Ethanol 15 mg/mL
In vitro
As a ATP-competitive inhibitor, AZD8055 can inihibit mTOR kinase with IC50 of 0.8 nM. AZD8055 shows inhibition to the phosphorylation of p70S6K and 4E-BP1, both of which are mTORC1 substrates. AZD8055 also can inhibit phosphorylation of the mTORC2 substrate AKT and downstream proteins. AZD8055 shows excellent selectivity (approximately 1,000-fold) against all class I phosphatidylinositol 3-kinase (PI3K) isoforms and other members of the PI3K-like kinase family. In vitro, AZD8055 potently inhibits proliferation and induces autophagy in H838 and A549 cells.AZD8055 induces a dose-dependent pharmacodynamic effect on phosphorylated S6 and phosphorylated AKT at plasma concentrations leading to tumor growth inhibition.
In vivo
In mice bearing U87-MG (PTEN null) glioblastoma xenografts, oral treatment with AZD8055 resulted in a dose-dependent tumor growth inhibition of 33%, 48%, and 77% with 2.5, 5, and 10 mg/kg/d twice daily, respectively. Antitumor activity in vivo induced by AZD8055 administered orally at a dose of 10 mg/kg twice daily or 20 mg/kg daily.
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