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RD162
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RD162图片
CAS NO:915087-27-3
规格:98%
分子量:476.4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
androgen receptor (AR) antagonist
CAS:915087-27-3
分子式:C22H16F4N4O2S
分子量:476.4
纯度:98%
存储:Store at -20°C

Background:

IC50: 30.9 nM


RD162 is an androgen receptor (AR) antagonist.


Metastatic prostate cancer is treated with drugs antagonizinf androgen action, but most patients progress to a more aggressive form of the disease named castration-resistant prostate cancer, driven by elevated expression of the androgen receptor (AR).


In vitro: RD162 was optimized from a screen for nonsteroidal antiandrogens retaining activity in the setting of increased androgen receptor expression. RD162 could bind to the androgen receptor with greater relative affinity than the clinically used bicalutamide, reduce the efficiency of the nuclear translocation, and impair both DNA binding to androgen response elements and recruitment of coactivators [1].


In vivo: Previous evidence suggested that the activity of RD162 in these mice was mediated through AR inhibition. The antitumor activity in the LNCaP/AR model was dose-dependent, with some slowing of tumor growth at 0.1 mg/kg RD162 and a few tumor regressions at 1 mg/kg, correlating closely with the effect of these same doses on AR transcriptional activity in the luciferase imaging experiment. In addition, neither bicalutamide nor RD162 impaired the growth of AR-negative DU145 prostate cancer xenografts [1].


Clinical trial: In a phase I/II clinical trial, of the first 30 patients treated with MDV3100, 13 (43%) showed sustained declines in serum concentrations of prostate-specific antigen, a biomarker of prostate cancer [1].


Reference:
[1] C.  Tran, S. Ouk, N. J. Clegg, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science 324(5928), 787-790(2009).