Bicalutimideisaninhibitoroftheandrogenreceptorthatexhibitsanticancerchemotherapeuticactivity.Withotheranti-androgens,bicalutimidedecreaseslevelsofBcl-2,Bcl-XL,caspase-3,andPARP,inducesapoptosis,andinhibitscellgrowthofprostatecancercells.Insimilaranimalmodels,thiscompounddecreasesplasmaPSAlevelsandsuppressestumorgrowth.Bicalutamidebindstheandrogenreceptorintwosites,distortingcoactivatorbindingandinhibitingtranscription.
| CasNo. | 90357-06-5 |
|---|---|
| Purity | ≥98% |
| Formula | C18H14F4N2O4S |
| FormulaWt. | 430.37 |
| ChemicalName | N-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methyl-,(+-)-Propanamide |
| IUPACName | N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide |
| Synonym | Casodex |
| MeltingPoint | 191-193°C |
| Solubility | Solubleinacetone,DMSO(86mg/m),ethanol(7mg/mL)orTHF.Slightlysolubleinchloroformorether.Practicallyinsolubleinwater. |
| Appearance | WhiteCrystalPowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| MSDS | B3209MSDSPDF |
|---|---|
| InfoSheet | B3209InfoSheetPDF |
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.
DeAmicisF,ThirugnansampanthanJ,CuiY,etal.Androgenreceptoroverexpressioninducestamoxifenresistanceinhumanbreastcancercells.BreastCancerResTreat.2010May;121(1):1-11.PMID:19533338.
