MK-2206（Akt inhibitor）

保质期 ：2 years

英文名 ：MK-2206（Akt inhibitor）

库存 ：10

供应商 ：上海伟进生物科技有限公司

CAS号 ：1032350-13-2

保存条件 ：-20℃

规格 ：5mg

Biological Activity

MK-2206 dihydrochloride is a highly potent and selective non-ATP competitive allosteric Akt inhibitor with IC₅₀’s of 5 nM, 12 nM and 65 nM for purified recombinant human Akt1, Akt2 and Akt3, respectively ^[1]. In vitro, MK-2206 synergistically suppresses cell proliferation of human cancer cell lines in combination with molecular targeted agents such as erlotinib (EGFR inhibitor) or lapatinib (EGFR /HER-2 inhibitor). In vivo, MK-2206 in combination with these anticancer agents significantly exerts more potent tumor inhibitory activities than each agent in the monotherapy setting ^[2]. 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 ^[3]. Treatment with MK-2206 causes a robust, concentration-dependent activation of autophagy in human glioma cell lines LN229 and T98G ^[4].

Chemical Properties

Cas No.: 1032350-13-2	M. Wt.: 480.39
Formula: C25H21N5O·2HCl	Purity: >98%
Chemical Name: 8-(4-(1-Aminocyclobutyl)phenyl-9-phenyl[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride
Appearance: A Crystalline solid
Solubility: Soluble in DMSO at 10 mg/mL.Very sparingly soluble in water.
Storage：Store solid at -20 ºC for the stability up to two years.