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  • Tariquidar methanesulfonate, hydrate

    • Tariquidar methanesulfonate hydrate,XR 9576,XR-9576
    货号: abs811447
    CAS号: 625375-83-9
    分子式: C40H52N4O15S2
    分子量: 892.99
    产品说明书
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    货号-规格 货期 价格 数量
    abs811447-10mg 4周 ¥950.00
    - +
    abs811447-50mg 4周 ¥2950.00
    - +
    大包装询价
    产品描述
    描述

    XR9576 is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in 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
    Tariquidar methanesulfonate hydrate,XR 9576,XR-9576
    可溶性/溶解性
    DMSO: ≥ 296 mg/mL; H2O: < 8.9 mg/mL
    生物活性
    靶点
    P-glycoprotein
    In vitro(体外研究)
    Tariquidar (XR9576) methanesulfonate is a potent modulator of P-gp mediated -Vinblastine and -Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CHrB30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC50=487±50 nM). -Tariquidar binds to CHrB30 membranes with the highest affinity (Kd=5.1±0.9 nM, n=7) and a binding capacity (Bmax) of 275±15 pmol/mg membrane protein. In contrast to the parental cell line, the accumulation of -Vinblastine is increased in a dose-dependent fashion by the modulators XR9576 (EC50=487±50 nM). The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity, with potent IC50 value of 43±9 nM. Tariquidar (XR9576) potentiates the cytotoxicity of several drugs including Doxorubicin, Paclitaxel, Etoposide, and Vincristine; complete reversal of resistance is achieved in the presence of 25-80 nM Tariquidar. Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by Azidopine implying a direct interaction with the protein.
    In vivo(体内研究)
    In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar (XR9576) methanesulfonate potentiates the antitumor activity of Doxorubicin without a significant increase in toxicity; maximum potentiation is observed at 2.5-4.0 mg/kg dosed either i.v. or p.o. In addition, coadministration of Tariquidar (6-12 mg/kg p.o.) fully restores the antitumor activity of Paclitaxel, Etoposide, and Vincristine against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. Tariquidar is found to also significantly potentiate the antitumor activity of doxorubicin against s.c. MC26 tumors in vivo.
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    • 实验方法 实验条件
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