2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. AR antagonist 9

AR antagonist 9 是一种具有口服活性的选择性 雄激素受体 (AR) 拮抗剂，通过破坏 AR 配体结合域二聚体的形成发挥抗癌作用，具有克服前列腺癌 (PCa) 药物抗性的潜力。其对 AR 的拮抗活性 IC50 为 0.051 μM，与 Enzalutamide (HY-70002) (IC50 = 0.060 μM) 相当。AR antagonist 9 对 ARF876L/T877A 和 ARW741C 突变体的抑制效果优于 Enzalutamide (HY-70002)。此外，AR antagonist 9 具有良好的药代动力学特性 (大鼠中的口服生物利用度 F = 66.24%)，在 LNCaP 异种移植小鼠模型中口服给药表现出显著的肿瘤生长抑制效果。AR antagonist 9 有望用于克服 PCa 抗药性领域的研究。

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AR antagonist 9 Chemical Structure

AR antagonist 9 Chemical Structure

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AR antagonist 9 相关抗体

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  • 生物活性

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生物活性

AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance[1].

分子量

351.29

Formula

C18H13F4NO2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AR antagonist 9 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AR antagonist 9AR antagonist9AR antagonist-9Androgen ReceptorInhibitorinhibitorinhibit

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