{"product_id":"m22384","title":"RD162","description":"\u003cp style=\"padding-left:1em;\"\u003eIC50: 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 .\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 915087-27-3\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 476.45\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C22H16F4N4O2S\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e 4-{7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl}-2-fluoro-N-methylbenzamide\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e CNC(=O)C1C=CC(=CC=1F)N1C(=S)N(C2C=C(C(=CC=2)C#N)C(F)(F)F)C(=O)C21CCC2\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e JPQFGMYHKSKKGW-UHFFFAOYSA-N\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e 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)\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eTechnical Data\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eAppearance:\u003c\/strong\u003e Solid Power\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003ePurity:\u003c\/strong\u003e ≥98% (or refer to the Certificate of Analysis)\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eShipping Condition:\u003c\/strong\u003e Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eStorage Condition:\u003c\/strong\u003e Dry, dark and -20 \u003csup\u003eo\u003c\/sup\u003eC for 1 year or refer to the Certificate of Analysis.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eShelf Life:\u003c\/strong\u003e ≥12 months if stored properly.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eStock Solution Storage:\u003c\/strong\u003e 0 - 4 \u003csup\u003eo\u003c\/sup\u003eC for 1 month or refer to the Certificate of Analysis.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eDrug Formulation:\u003c\/strong\u003e To be determined\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eHS Tariff Code:\u003c\/strong\u003e 382200\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"Xcess Biosciences","offers":[{"title":"M22384-C \/ Contact sales@xcessbio.com for quotation","offer_id":39527422754955,"sku":"0","price":100.0,"currency_code":"USD","in_stock":false}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/products\/M22384_1635323070.gif?v=1635323072","url":"https:\/\/www.xcessbio.com\/products\/m22384","provider":"Xcess Biosciences","version":"1.0","type":"link"}