MK-2206, a highly selective non-ATP competitive allosteric Akti, has nM IC50 and broad preclinical antitumor activity. [1] 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. [1] 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 should at 60 mg. [2]
珠海市活力達生物科技有限公司
聯(lián)系商家時請?zhí)峒癱hemicalbook,有助于交易順利完成!