mTOR Kinase Inhibitor II, WYE-354

A cell-permeable pyrazolopyrimidine compound that acts as a potent and ATP-competitive mTOR inhibitor (IC₅₀ = 5 nM with S6K as the substrate and 100 µM ATP) with much reduced activity against PI 3-Kα or PI 3-Kγ (IC₅₀ = 1.89 and 7.37 µM, respectively) and little or no activity toward 24 other kinases (IC₅₀ >50 µM). WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC₅₀<200 nM; [ATP] = 100 µM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Yu, K., et al. 2009. Cancer Res.69, 6232.
Zask, A., et al. 2009. J. Med. Chem.52, 5013.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)