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当前位置: 首页 > 信号通路研究 > Androgen Receptor > AZD3514
AZD3514
AZD3514
AZD3514
商品货号:CL-10971
CAS 号:1240299-33-5
英文名字:AZD3514
质量标准:>98%,androgen receptor抑制剂
分子式:C25H32F3N7O2
  • 包装规格:
    规格 库存 发货时间
    50mg [¥6060.00]15 现货,一周内发货
    100mg [¥9930.00]15 现货,一周内发货
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    商品信息

    质检证书(coa)

    说明书下载

     AZD-3514

    分子式C25H32F3N7O2   分子量519.56

     

    产品描述

    AZD3514是口服的有效 androgen receptor抑制剂,Ki2.2 μM,且降低AR蛋白表达。

    靶点

    Androgen Receptor

             

    IC50

    2.2 μM (Ki)

             

    体外研究

    AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors. In vitro AZD3514 inhibits cell growth in prostate cancer cells expressing wild-type (VCaP) and mutated (T877A) AR (LNCaP), but is inactive in AR-negative prostate cancer cells. AZD3514 causes a rapid reduction in PSA synthesis in vitro; with a significant decrease in PSA mRNA being evident in LNCaP cells within 2-3 h of compound treatment. AZD3514 inhibits an androgen-induced translocation of AR from the cytoplasm to the nucleus within a comparable time-frame in LNCaP cells and U2OS AR-transfected cells. AZD3514 treatment also reduces AR protein in LNCaP cells maintained in steroid-depleted conditions; an effect which is evident within 6-8 h, and maximal at 18-24 h. The ability to down-regulate AR under such conditions differentiates AZD3514 from the AR antagonists bicalutamide and Enzalutamide, which do not reduce AR protein levels.

    体内研究

    Oral administration of AZD3514 (100mg/kg once-daily for 7 days) significantly inhibits testosterone-induced growth of sexual accessory organs. The mode of action of AZD3514 is associated with loss of AR function. Administration of AZD3514 (100 mg/kg/day orally) for 3 days to Copenhagen rats bearing R3327H Dunning prostate tumours, indicates that AZD3514 treatment also reduces tumour AR in vivo.

    溶解性

    DMSO 100 mg/mL,水 <1 mg/mL,乙醇 100 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

           
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