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  • AZD-7762

    • AZD7762;AZD-7762
    货号: abs810415
    CAS号: 860352-01-8
    分子式: C17H19FN4O2S
    分子量: 362.42
    产品说明书
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    货号-规格 货期 价格 数量
    abs810415-5mg 现货 ¥942.00
    - +
    abs810415-10mg 现货 ¥1450.00
    - +
    abs810415-50mg 现货 ¥4233.00
    - +
    abs810415-100mg 现货 ¥7619.00
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    大包装询价
    产品描述
    描述

    AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM; equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.

    纯度
    >98%
    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.
    基本信息
    别名
    AZD7762;AZD-7762
    外观
    White to off-white powder
    可溶性/溶解性
    DMSO : 47 mg/mL (129.7 mM)
    生物活性
    靶点
    Chk1;Chk2
    In vitro(体外研究)
    AZD7762, a more selective Chk1 inhibitor, inhibits Chk1 phosphorylation of a cdc25C peptide by reversibly binding to the ATP-binding site of Chk1, with IC50 of 5 nM and Ki of 3.6 nM. AZD7762 induces cell arrest with EC50 of 0.620 μM, and significantly abrogates the camptothecin induced G2 arrest with an EC50 of 10 nM, by blocking the chk1 dependent degradation of Cdc25A and activation of Cyclin A. AZD7762 (300 nM) enhances the antitumor efficacy of gemcitabine against SW620 and topotecan against MDA-MB-231 by reducing the GI50 values from 24.1 nM and 2.25 μM to 1.08 nM and 0.15 μM, respectively. AZD7762 shows cytotoxicity against a variety of neuroblastoma cell lines bearing p53 wild type, p53 mutation, Mdm2 amplification or p14 deletion with IC50 values ranging from 82.6-505.9 nM.
    In vivo(体内研究)
    AZD7762 alone at 25 mg/kg shows little antitumor activity in the H460-DNp53 xenograft mice and SW620 xenograft mice, but when administrated in combination with gemcitabine (60 mg/kg), AZD7762 shows significant antitumor efficacy in the two xenografts mice with a log cell kill of 0.9 or percent treated/control (%T/C) of 26 even at low dose of 12.5 mg. Dosing of AZD7762 in combination with gemcitabine (10 mg/kg) in the H460-DNp53 xenograft rat inhibits the tumor volume in a dose-dependent manner with the %T/C values of 48 and 32 for 10 and 20 mg/kg AZD7762, respectively. AZD7762 (25 mg/kg) in combination with irinotecan (25 or 50 mg/kg) causes complete tumor regression in the SW620 xenograft mice with the %T/C increasing significantly to -66% and -67%, respectively.
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