Cayman PKI-402

PKI-402 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC₅₀s = 1.4, 9.2, and 1.7 nM for PI3Kα, PI3Kγ, and mTOR, respectively). It reduces proliferation of MDA-MB-361 and PC3 cancer cells (IC₅₀s = 8 and 21 nM, respectively) and inhibits phosphorylation of Akt in MDA-MB-361 cells (IC₅₀ = 5 nM). PKI-402 (25, 50, and 100 mg/kg) reduces intratumor phosphorylation of Akt and tumor growth in an MDA-MB-361 mouse xenograft model. It also inhibits tumor growth in U87MG glioma and A549 lung cancer mouse xenograft models in a dose-dependent manner.

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