WYE-125132 (WYE-132) is a potent, specific, ATP-competitive and orally active mTOR inhibitor with IC50 of 0.19 nM.
WYE-125132 dispalys high selectivity (>5,000-fold) over PI3Ks, the PI3K-related kinases hSMG1 and ATR, and a panel of 230 protein kinases.
WYE-125132 inhibits mTORC1-dependent phosphorylation of S6K(T389) and mTORC2-dependent phosphorylation of AKT(S473), inhibits cancer cell proliferation, cell cycle progression, and induces apoptosis.
WYE-125132 shows potent single-agent antitumor activity against multiple cancer models.
