PKI-402

A dual inhibitor of PI3K and mTOR (IC50s = 1.4, 9.2, and 1.7 nM for PI3Kα, PI3Kγ, and mTOR, respectively); reduces proliferation of MDA-MB-361 and PC3 cancer cells (IC50s = 8 and 21 nM, respectively); inhibits phosphorylation of Akt in MDA-MB-361 cells (IC50 = 5 nM); reduces intratumor phosphorylation of Akt and tumor growth in an MDA-MB-361 mouse xenograft model at 25, 50, and 100 mg/kg; inhibits tumor growth in U87MG glioma and A549 lung cancer mouse xenograft models