mTOR Kinase Inhibitor II, WYE-354-CAS 1062169-56-5-Calbiochem

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一般描述

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 ?M ATP) with much reduced activity against PI 3-Kα or PI 3-Kγ (IC₅₀= 1.89 and 7.37 ?M, respectively) and little or no activity toward 24 other kinases (IC₅₀>50 ?M). 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 ?M) 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.

包装

5 mg in Plastic ampoule
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

法律信息

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

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