RD162

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

RD162 

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。

RD162

RD162 Chemical Structure

CAS No. : 915087-27-3

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生物活性

RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer[1].

体外研究
(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[1].
RD162 has little to no binding to the progesterone, estrogen or glucocorticoid receptors in an in vitro fluorescence polarization assay[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: VCaP cells
Concentration: 1, 10 μM
Incubation Time: 4 days
Result: Suppressed cell growth.

体内研究
(In Vivo)

RD162 (10 mg/kg; oral gavage; daily; for 28 days) causes all tumors regressed[1].
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[1].
RD162 (20 mg/kg; gavage) is ∼50 percent bioavailable after oral delivery with a serum half-life of about 30 hours[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Castrate male mice bearing LNCaP/AR xenografts[1]
Dosage: 10 mg/kg
Administration: Oral gavage; daily; for 28 days
Result: Caused all tumors regressed.
Animal Model: Male mice[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage (in 0.5% hydroxy-methyl-propyl-cellulose)
Result: Had ∼50 percent bioavailable after oral delivery with a serum half-life of about 30 hours.

分子量

476.45

Formula

C22H16F4N4O2S

CAS 号

915087-27-3

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.

参考文献
  • [1]. Chris Tran, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90.

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