PKI-179 is a cell-permeable triazinyl-phenyl-pyridinylurea compound that acts as a potent inhibitor against mTOR (IC50 = 0.42 nM) and PI 3-K (IC50 = 8, 24, 74, 77, 14, and 11 nM against isoform α, β, γ, δ, α E545K mutant, and α H1047R mutant, respectively) activities, exhibiting much reduced or little activity against a panel of 361 other kinases (IC50 >50 μM), Cytochrome CYP isoforms, or hERG. PKI-179 is reported to effectively suppress cancer growth in cultures in vitro (IC50 = 22 and 29 nM, respectively, against MDA361 and PC3mm2) via apoptosis induction as a result of Akt/mTOR pathway inhibition.