RD162

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 . 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 . 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 .

Product information

CAS Number: 915087-27-3

Molecular Weight: 476.45

Formula: C22H16F4N4O2S

Chemical Name: 4-{7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl}-2-fluoro-N-methylbenzamide

Smiles: CNC(=O)C1C=CC(=CC=1F)N1C(=S)N(C2C=C(C(=CC=2)C#N)C(F)(F)F)C(=O)C21CCC2

InChiKey: JPQFGMYHKSKKGW-UHFFFAOYSA-N

InChi: InChI=1S/C22H16F4N4O2S/c1-28-18(31)15-6-5-14(10-17(15)23)30-20(33)29(19(32)21(30)7-2-8-21)13-4-3-12(11-27)16(9-13)22(24,25)26/h3-6,9-10H,2,7-8H2,1H3,(H,28,31)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.