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  • Atrasentan hydrochloride

    • ABT-627, ABT627, ABT 627
    货号: abs811604
    CAS号: 195733-43-8
    分子式: C29H39ClN2O6
    分子量: 547.08
    产品说明书
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    货号-规格 货期 价格 数量
    abs811604-10mg 4周 ¥3791.00
    - +
    abs811604-50mg 4周 ¥10219.00
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    大包装询价
    产品描述
    描述

    Atrasentan hydrochloride is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer.

    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
    ABT-627, ABT627, ABT 627
    可溶性/溶解性
    10 mM in DMSO
    生物活性
    靶点
    Endothelin Receptor
    In vitro(体外研究)
    Atrasentan (ABT-627, 0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. ABT-627 in conbination with Taxotere elicits a significantly greater loss of viable prostate cancer cells relative to either agent alone and shows greater degree of down-regulation of the NF-κB DNA binding activity. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC50 in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells=59.8±11 μM).
    In vivo(体内研究)
    Atrasentan (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats. Aatrasentan (ABT-627, 10 mg/kg, i.p.) as well as Taxotere alone inhibited the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model.
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    • 实验方法 实验条件
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