Akt Inhibitor XVI, AT7867-Calbiochem

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一般描述

A cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC₅₀= 32, 17, and 47 nM against Akt1, Akt2, and Akt3, respectively), PKA (IC₅₀= 20 nM), and p70S6K (IC₅₀= 85 nM) in an ATP-competitive manner (K_i= 18 nM using AKT2), with much reduced potency toward RSK1 (IC₅₀>100 nM) and a panel of 13 other cellular kinases (IC₅₀>1 ?M). Shown to reduce cellular phosphorylation of GSK-3β (IC₅₀range from 2.08 to 4.45 ?M), S6R, FKHRL1, and inhibit the proliferation of cancer cells exhibiting constitutive Akt pathway activation bothin vitro(IC₅₀range from 0.94 to 11.86 ?M) and in micein vivo(20 mg/kg via i.p. or 90 mg/kg via p.o.).
A cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC₅₀= 32, 17, and 47 nM against Akt1, Akt2, and Akt3, respectively), PKA (IC₅₀= 20 nM), and p70S6K (IC₅₀= 85 nM) in an ATP-competitive manner (K_i= 18 nM using AKT2), with much reduced activity toward RSK1 (IC₅₀>100 nM) and a panel of 13 other cellular kinases (IC₅₀>1 ?M), including PDK1, PI 3-Kβ, SGK, GSK-3β, and MEK1. Shown to effectively reduce the phosphorylation levels of GSK-3β, S6R, and FKHRL1 (IC₅₀range from 2.08 to 4.45 ?M against GSK-3β pSer⁹level), as well as inhibit the proliferation (IC₅₀range from 0.94 to 11.86 ?M) of cancer cells exhibiting constitutive Akt pathway activation, including thePTEN-deficient MES-SA uterine sarcoma and U87MG glioblastoma cell lines. AT7867 treatments via i.p. or p.o. (20 mg/kg and 90 mg/kg, respectively, once every 3 days) are also reported to result in Akt pathway and tumor growth inhibition in mice bearing MES-SA (~40% of untreated control on day 10 by i.p. or p.o.) or U87MG (~50% of untreated control on day 10 by i.p.) xenograftin vivo.

包装

10 mg in Glass bottle
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 3 months at -20°C.

其他说明

Grimshaw, K.M., et al. 2010.Mol. Cancer Ther.9,1100.
Saxty, G., et al. 2007.J. Med. Chem.50,2293.

法律信息

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

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