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  • AZD9496
    • AZD-9496, AZD 9496
    货号: abs811862
    CAS号: 1639042-08-2
    分子式: C25H25F3N2O2
    分子量: 442.48
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs811862-5mg 1-2周 ¥1577.00
    - +
    abs811862-10mg 1-2周 ¥2790.00
    - +
    大包装询价
    产品描述
    描述

    AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator and antagonist.

    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
    AZD-9496, AZD 9496
    外观
    Solid powder
    可溶性/溶解性
    DMSO: ≥ 104.5 mg/mL
    生物活性
    靶点
    estrogen receptor
    In vitro(体外研究)
    AZD9496 showed pmol/L equipotent binding to both ERα and ERβ isoforms. AZD9496 directly targets ERα for downregulation in vitro. And it also antagonizes and downregulates mutant ER in vitro and in vivo. The IC50s of ERα binding, ERα downregulation, ERα antagonism for AZD9496 are 0.82, 0.14 and 0.28 nM, respectively.
    In vivo(体内研究)
    AZD9496 showed high oral bioavailability across three species (F% 63, 91, and 74, rat, mouse, and dog, respectively) with generally low volume and clearance across species, albeit a higher clearance in mouse. The percent free levels in human plasma of 0.15% were 5-fold higher than those measured for fulvestrant. AZD9496 is a potent, oral inhibitor of breast tumor growth in vivo. AZD9496 causes tumor regressions in combination with PI3K pathway and CDK4/6 inhibitors and in an estrogen-deprived ER+ model of resistance. This effect was accompanied by a dose-dependent decrease in PR protein levels. AZD9496 is currently being evaluated in a phase I clinical trial.
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