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  • Bicalutamide

    • 比卡鲁胺
    货号: abs817935
    CAS号: 90357-06-5
    分子式: C18H14F4N2O4S
    分子量: 430.37
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    货号-规格 货期 价格 数量
    abs817935-50mg 现货 ¥497.00
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    abs817935-100mg 现货 ¥744.00
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    abs817935-500mg 现货 ¥2040.00
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    大包装询价
    产品描述
    描述

    Bicalutamide 是非甾体抗雄激素化合物,能与雄激素受体结合,可作用于前列腺癌,IC50为0.16 μM。

    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
    比卡鲁胺
    外观
    White powder
    可溶性/溶解性
    DMSO : ≥ 50 mg/mL (116.18 mM)
    生物活性
    靶点
    Androgen Receptor
    In vitro(体外研究)
    Bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity. Bicalutamide treatment of LNCaP/AR(cs) cells in absence of the synthetic androgen R1881 results in altered gene expression consistent with its well-documented agonist activity in context of AR overexpression. Bicalutamide induces cell proliferation in a dose-dependent manner, and only partially antagonized the effects of R1881. Bicalutamide treatment also results in a significant amount of nuclear AR, although less than that observed with R1881. Bicalutamide exhibits partial agonist activity as evidenced by induction of DNA binding at AR target genes and incomplete antagonism of the effects of R1881. In absence of R1881, Bicalutamide partially activates VP16-AR–mediated transcription, indicative of AR binding to DNA. In LNCaP/AR-luc cells with a stably integrates AR-driven luciferase reporter construct. In the presence of R1881, Bicalutamide shows only weak partial antagonism of VP16-AR–mediated transcription with an IC50 of 0.35 μM. Micromolar bicalutamide causes a significant dose-dependent reduction in clonogenicity. Dual inhibition of the AR and mTOR signaling pathways provides further benefit with the ridaforolimus-bicalutamide combination producing syner -gistic antiproliferative effects in prostate cancer cells in vitro when compared with each agent alone.
    In vivo(体内研究)
    Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-bicalutamide combination exhibits improved and potent antitumor activity, almost completely abrogating tumor growth. The combination is also well tolerated, as evidenced by no significant changes in body weight over the course of treatment. Plasma PSA levels are again tightly linked to tumor growth in the combination-treated mice.
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    • 实验方法 实验条件
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