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Elacestrant dihydrochloride,1349723-93-8

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    YZ剂描述:

    产品名称:Elacestrant dihydrochloride

    产品别名:见爱必信官网

    英文别名:Elacestrant dihydrochloride

    靶点:Estrogen Receptor_ERR

    CAS:1349723-93-8

    纯度:见爱必信官网

    外观:见爱必信官网

    保存方法:见爱必信官网

    描述:Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.

    溶解性:DMSO: 17.6 mg/mL; H2O

    体外研究:

    RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation. RAD1901 treatment exhibits dose-dependent inhibition of ERα expression, with an EC50 of 0.6 nM. Treatment of ER-positive MCF-7 cells with E2 results in a potent and dose-dependent increase in proliferation, with an EC50 of 4 pM. Treatment of cells with RAD1901 in the presence of 10 pM E2 resultsin a dose-dependent decrease in proliferation, with an IC50 value of 4.2 nM.

    体内研究:RAD1901 produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models. RAD1901-treated animals survived longer than those treated with either control or fulvestrant. RAD1901 preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2.

    产品信息订购:

      产品货号   产品名称   规格 价格 大包装及货期
      abs819060   Elacestrant dihydrochloride   1mg  2400   立即咨询

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