R-Bicalutimideisaninhibitoroftheandrogenreceptorthatexhibitsanticancerchemotherapeuticactivity.Withotheranti-androgens,R-bicalutimidedecreaseslevelsofBcl-2,Bcl-XL,caspase-3,andPARP,inducesapoptosis,andinhibitscellgrowthofprostatecancercells.Insimilaranimalmodels,thiscompounddecreasesplasmaPSAlevelsandsuppressestumorgrowth.Bicalutamidebindstheandrogenreceptorintwosites,distortingcoactivatorbindingandinhibitingtranscription.Opticalrotation:[a]20D=-83.~–85.0(C=1,MeOH)
| CasNo. | 113299-40-4 |
|---|---|
| Purity | ≥98% |
| Formula | C18H14F4N2O4S |
| FormulaWt. | 430.37 |
| ChemicalName | R-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methyl-,(+-)-Propanamide |
| IUPACName | (2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide |
| MeltingPoint | 178-179°C |
| Solubility | water:5mg/L |
| Appearance | WhiteCrystallinepowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | B3210InfoSheetPDF |
|---|
SquillaceRM,MillerD,WardwellSD,etal.SynergisticactivityofthemTORinhibitorridaforolimusandtheantiandrogenbicalutamideinprostatecancermodels.IntJOncol.2012Aug;41(2):425-32.PMID:22614157.
YanJ,XieB,CapodiceJL,etal.Zyflamendinhibitstheexpressionandfunctionofandrogenreceptorandactssynergisticallywithbicalutimidetoinhibitprostatecancercellgrowth.Prostate.2012Feb;72(3):244-52.PMID:21656835.
