AMG511 (AMG-511) potent, efficacious, and orally available pan class I PI3K inhibitor with Ki of 4/6/2/1 nM for PI3Kα/β/δ/γ, respectively.
AMG511 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>1 uM).
AMG511 inhibits AKT (Ser473) phosphorylation in U87 MG glioblastoma cells with IC50 of 4 nM.
AMG511 potently blocks the targeted PI3K pathway in mouse liver pharmacodynamic model and inhibits tumor growth in U87 malignant glioma glioblastoma xenograft model.
