WYE-687

WYE-687 is an inhibitor of mammalian target of rapamycin (mTOR; IC₅₀ = 0.007 µM).¹ 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.²

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1. Yu, K., Toral-Barza, L., Shi, C., et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 69(15), 6232-6240 (2009).

2. Cheng, F., Wang, L., Shen, Y., et al. Preclinical evaluation of WYE-687, a mTOR kinase inhibitor, as a potential anti-acute myeloid leukemia agent. Biochem. Biophys. Res. Commun. 470(2), 324-330 (2016).