Description
A potent, efficacious, and orally available pan class I PI3K inhibitor with Ki of 4/6/2/1nM for PI3Kalpha/beta/delta/gamma, respectively; displays high selectivity over other members of the closely related PIKK family of kinases, including mTOR, hVPS34 and PI4Ks, as well as a panel of 370 protein kinases (IC50>1uM); inhibits AKT (Ser473) phosphorylation in U87mg glioblastoma cells with IC50 of 4nM; potently blocks the targeted PI3K pathway in mouse liver pharmacodynamic model and inhibits tumor growth in U87 malignant glioma glioblastoma xenograft model