A-674563CAS号: 552325-73-2分子式: C22H22N4O分子量: 358.44描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
产品描述 | |
描述 |
A-674563 is a potent and selective Akt1 inhibitor with a Ki of 11 nM. |
纯度 |
≥98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
A 674563;A674563
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外观 |
White to off-white powder
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可溶性/溶解性 |
DMSO :72 mg/mL (200.87 mM)
Water :72 mg/mL (200.87 mM) Ethanol :18 mg/mL (50.21 mM) |
生物活性 | |
靶点 |
Akt1,PKA,CDK2,GSK-3β,ERK2
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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.
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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.
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参考文献 | |
参考文献 |
[1] Zhu QS, et al, Cancer Res, 2008, 68(8), 2895-2903. |
分子结构图