PKI-402 is a dual inhibitor targeting PI3K and mTOR (IC50s of 1.4, 9.2, and 1.7 nM respectively). It curbs proliferation of MDA-MB-361 and PC3 cancer cells (IC50s of 8 and 21 nM) and blocks Akt phosphorylation in MDA-MB-361 cells (IC50 of 5 nM). In vivo, PKI-402 (25, 50, and 100 mg/kg) reduces Akt phosphorylation and tumor growth in MDA-MB-361 mouse models, and inhibits tumor growth in U87MG glioma and A549 lung cancer models in a dose-dependent manner.
