WYE-687 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.007 uM).{17537} It is selective for mTOR over PI3Ka and PI3Ky (IC50s = 0.81 and 3.11 uM, respectively), as well as a panel of 24 additional kinases (IC50s = >50 uM for all). WYE-687 (0.2, 1, and 5 uM) 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 uM. 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}
5 mg
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Cayman Chemical
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