| CAS NO: | 915087-27-3 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at 4°C |
| M.Wt | 476.4 |
| Cas No. | 915087-27-3 |
| Formula | C22H16F4N4O2S |
| Solubility | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | 4-[7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide |
| Canonical SMILES | S=C1N(C2=CC=C(C#N)C(C(F)(F)F)=C2)C(C3(CCC3)N1C4=CC(F)=C(C(NC)=O)C=C4)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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).
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