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WAY-600 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.009 µM).1 It selectively inhibits mTOR over PI3Kα and PI3Kɣ (IC50s = 1.96 and 8.45 µM, respectively) and 24 additional lipid and protein kinases in a panel (IC50s = >50 µM for all). WAY-600 decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1), respectively, in a cell-free assay when used at concentrations of 0.2, 1, and 5 µM. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.6 to 2.5 µM. WAY-600 reduces tumor growth in a HepG2 mouse xenograft model when administered at a dose of 10 mg/kg for 14 days.2
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1. Biochemical, cellular, and in vivo activity of novel ATP-
2. MEK-