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  • A-674563
    • A 674563;A674563
    货号: abs812083
    CAS号: 552325-73-2
    分子式: C22H22N4O
    分子量: 358.44
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs812083-2mg 1-2周 ¥1274.00
    - +
    abs812083-5mg 1-2周 ¥2202.00
    - +
    abs812083-10mg 1-2周 ¥3439.00
    - +
    大包装询价
    产品描述
    描述

    A-674563 is a potent and selective Akt1 inhibitor with a Ki of 11 nM. 

    纯度
    ≥98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    A 674563;A674563
    外观
    White to off-white powder
    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
    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.
    参考文献
    参考文献
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