产品信息
抗原名称
Akt1,PKA,CDK2,GSK-3β,ERK2
商品描述
A-674563 is a potent and selective Akt1 inhibitor with a Ki of 11 nM.
分子量
358.44
纯度
≥98%
可溶性
DMSO ：72 mg/mL (200.87 mM)
Water ：72 mg/mL (200.87 mM)
Ethanol ：18 mg/mL (50.21 mM)
Water ：72 mg/mL (200.87 mM)
Ethanol ：18 mg/mL (50.21 mM)
外观
White to off-white powder
In vitro(体外研究)
A-674563 is achieved from A-443654 by replacing the indole with a phenyl moiety and getting oral activity. A-674563 slows proliferation of tumor cells with EC50 of 0.4 μM. A-674563 does not inhibit Akt phosphorylation per se, but blocks the phosphorylation of Akt downstream targets in a dose-dependent manner. A-674563 induced Akt blockade results in decreased STS cell downstream target phosphorylation and tumor cell growth inhibiton. A-674563 induces G2 cell cycle arrest and apoptosis in STS cells.
In vivo(体内研究)
20 mg/kg A-674563 increases plasma insulin in an oral glucose tolerance test. A-674563 shows no significant monotherapy tumor inhibitory activity; the efficacy of the combination therapy is significantly improved compared to paclitaxel monotherapy. A674563-treated (20 mg/kg/bid, p.o.) mice exhibits slower tumor growth and more than 50% decrease in the tumor volume at the termination of the study compared with that in control group. A-674563 is identified to have drastically improved PK profile with oral bioavailability of 67% in mouse, but is 70-fold less active than A-443654.
背景
别名
A 674563；A674563
分子式
C22H22N4O
CAS号
552325-73-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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