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AR antagonist 9 是一种口服活性选择性雄激素受体 (AR) 拮抗剂,通过破坏AR配体结合域的二聚体形成来发挥抗癌作用,具有潜在克服前列腺癌 (PCa) 药物抗性的能力。其拮抗AR的活性IC50为0.051 μM,与Enzalutamide的IC50=0.060 μM相当。相比Enzalutamide,AR antagonist 9 对ARF876L/T877A和ARW741C突变体表现出更强的抑制效果。此外,该化合物在药代动力学特性方面表现优良 (在大鼠中的口服生物利用度F = 66.24%),通过口服给药在LNCaP异种移植小鼠模型中显示出显著的肿瘤生长抑制效果。AR antagonist 9 有望成为克服PCa抗药性领域的重要研究对象。
AR antagonist 9 是一种口服活性选择性雄激素受体 (AR) 拮抗剂,通过破坏AR配体结合域的二聚体形成来发挥抗癌作用,具有潜在克服前列腺癌 (PCa) 药物抗性的能力。其拮抗AR的活性IC50为0.051 μM,与Enzalutamide的IC50=0.060 μM相当。相比Enzalutamide,AR antagonist 9 对ARF876L/T877A和ARW741C突变体表现出更强的抑制效果。此外,该化合物在药代动力学特性方面表现优良 (在大鼠中的口服生物利用度F = 66.24%),通过口服给药在LNCaP异种移植小鼠模型中显示出显著的肿瘤生长抑制效果。AR antagonist 9 有望成为克服PCa抗药性领域的重要研究对象。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 期货 | |
50 mg | 询价 | 期货 |
产品描述 | AR antagonist 9 is an orally active, selective androgen receptor (AR) antagonist that inhibits cancer by disrupting the formation of AR ligand-binding domain dimers, showing potential in overcoming drug resistance in prostate cancer (PCa). Its antagonistic activity against AR has an IC50 of 0.051 μM, comparable to Enzalutamide (IC50= 0.060 μM). This compound demonstrates superior inhibitory effects on ARF876L/T877A and ARW741C mutants compared to Enzalutamide. Additionally, AR antagonist 9 possesses favorable pharmacokinetic properties, with an oral bioavailability (F) of 66.24% in rats, and significantly inhibits tumor growth in LNCaP xenograft mouse models upon oral administration. AR antagonist 9 holds promise for research in overcoming PCa resistance. |
分子量 | 351.29 |
分子式 | C18H13F4NO2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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