产品描述:
WYE-687 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.007 µM).{17537} It is selective for mTOR over PI3Kα and PI3Kγ (IC50s = 0.81 and 3.11 µM, respectively), as well as a panel of 24 additional kinases (IC50s = >50 µM for all). WYE-687 (0.2, 1, and 5 µM) decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1) in a cell-free assay. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.18 to 1.25 µM. WYE-687 inhibits survival of HL-60 and U937 leukemia cells in a concentration-dependent manner and reduces tumor growth in a U937 mouse xenograft model when administered at doses of 5 and 25 mg/kg.{53480}