MK-2206/MK2206

溶解度:DMSO

储存条件:Storage at -20C 2 years

生物活性

MK-2206, a highly selective non-ATP competitive allosteric Akti, has nM IC50 and broad preclinical antitumor activity.MK-2206 is a potent allosteric Akt inhibitor with IC50 at 8 nm, 2 mM, 65 mM for Akt1, Akt2 and Akt3 respectively. 1 hr treatment of 1 µM MK-2206 abolished Akt phosphorylation in U87MG cells. MK-2206 treatment abolished IR-induced Akt phosphorylation. Moreover, treatment with MK-2206 also increased the radiosensitivity of U87MG cells.MK-2206 is generally well tolerated at doses up to 60 mg QOD with plasma concentrations that portend activity in preclinical models. PK/PD data suggest a substantial and maintained target inhibition at 60 mg.

参考文献

1. Hui-Fang Li , Jung-Sik Kim , Todd Waldman. Radiation-induced Akt activation modulates radioresistance in human glioblastoma cells Radiation Oncology 2009, 4:43 2. A. W. Tolcher . A phase I study of MK-2206, an oral potent allosteric Akt inhibitor (Akti), in patients (pts) with advanced solid tumor (ST). Meeting: 2009 ASCO Annual Meeting