RD162

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RD162

CAS No. : 915087-27-3

MCE 国际站：RD162

产品活性：RD162 是一种二芳基硫代乙内酰脲，一种口服有效的非甾体抗雄激素 (NSAA)。RD162 与雄激素受体 (AR) 特异性结合。RD162 在去势抵抗人前列腺癌小鼠模型中诱导肿瘤消退。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Androgen Receptor

In Vitro: RD162 (1-10 μM; 4 days) suppresses growth and induces apoptosis in the human prostate cancer cell line VCaP which has endogenous AR gene amplification.
RD162 has little to no binding to the progesterone, estrogen or glucocorticoid receptors in an in vitro fluorescence polarization assay.

In Vivo: RD162 (10 mg/kg; oral gavage; daily; for 28 days) causes all tumors regressed.
RD162 (0.1, 1, 10 mg/kg; oral gavage; daily; for 5 days) consistently reduces luciferase activity with 10 mg/kg/day human LNCaP/AR xenografts grown in castrated male mice whereas lower doses of 0.1 and 1.0 mg/kg/day has minimal effect. RD162 substantially reduces cellular proliferation after 5 days.
RD162 (20 mg/kg; gavage) is ∼50 percent bioavailable after oral delivery with a serum half-life of about 30 hours.

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