PP-242 is a selective mTOR inhibitor with IC50 of 8 nM. mTOR has emerged as an important drug target, and PP-242 is the first selective and ATP competitive inhibitor of mTOR that has been described. Unlike rapamycin, PP-242 inhibits both mTORC1 and mTORC2. PP-242 suppresses bladder cancer cell proliferation and migration through deactivating the mammalian target of rapamycin complex 2/AKT1 signaling pathway. PP242 also inhibits several protein kinases including PKC, RET and JAK2 kinases. PP-242 shows strong antitumor activity in a pheochromocytoma PC12 cell tumor model. PP-242 suppresses cell proliferation, metastasis, and angiogenesis of gastric cancer through inhibition of the PI3K/AKT/mTOR pathway. PP-242 induces apoptosis in AML cells under conditions mimicking the bone marrow microenvironment.