现货供应MK-2206
产品型号:C13900
英文简称:
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产品详情
别名:MK-2206;MK2206
分子式:C25H23Cl2N5O
分子量:480.39
外观:White solid
纯度:>99%
CAS:1032350-13-2
Biological Activity:
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.