PKI-402 is a potent dual PI3K/mTOR inhibitor with IC50 of 1/7/16/14/1.7 nM for PI3Kα/β/γ/δ/mTOR respectively.
PKI-402 shows excellent suppression of Akt T308 phosphorylation (IC50=5 nM), and excellent inhibition of cell proliferation in several human cancer cell lines.
PKI-402 shows excellent in vivo efficacy in various human cancer xenografts, good physical properties and PK parameters.
