Enzalutamideisanandrogen-receptor(AR)antagonistwithIC₅₀of36nMinLNCaPcells.

IC50:36nM(androgen-receptor,inLNCaPcells)^[1]

EnzalutamidehasgreateraffinitytoARthanBicalutamidedoesinacompetitionassaywith16β-[¹⁸F]fluoro-5α-DHT(18-FDHT)incastration-resistantLNCaP/ARcells(AR-overexpressing).WhileEnzalutamideshowsnoagonisminLNCaP/ARprostatecells.Enzalutamideantagonizesinductionofprostate-specificantigen(PSA)andtransmembraneserineprotease2(TMPRSS2),combinationwiththesyntheticandrogenR1881inparentalLNCaPcells.EnzalutamideinhibitsthetranscriptionalactivityofamutantARprotein(W741C,mutationofTrp741toCys)^[1].Enzalutamidealsopreventsnucleartranslocationandco-activatorrecruitmentoftheligand-receptorcomplex^[2].

EnzalutamideinducesgreattumorregressionincastratemalemicebearingLNCaP/ARxenograftsatadoseof10mg/kg^[1].Enzalutamideshowsdose-independentpharmacokineticsatintravenousandoraldosesof0.5-5mg/kg^[4].

• [1].TranC,etal.Developmentofasecond-generationantiandrogenfortreatmentofadvancedprostatecancer.Science,2009,324(5928),787-790.

  [2].ScherHI,etal.AntitumouractivityofMDV3100incastration-resistantprostatecancer:aphase1-2study.Lancet,2010,375(9724),1437-1446.

  [3].GuerreroJ,etal.Enzalutamide,anandrogenreceptorsignalinginhibitor,inducestumorregressioninamousemodelofcastration-resistantprostatecancer.Prostate.2013Sep;73(12):1291-305.

  [4].KimTH,etal.Pharmacokineticsofenzalutamide,ananti-prostatecancerdrug,inrats.ArchPharmRes.2015Nov;38(11):2076-82.

EnzalutamideisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse^[1].

LNCaPcells(10⁷cells/condition)aregrowninRPMImediasupplementedwith5%charcoalstrippedserumfor22days,thentreatedwithDMSOor1nMR1881,combinedwithanantiandrogen(DMSO,1μMBicalutamide,10μMBicalutamide,1μMRD162,10μMRD162,1μMMDV3100,or10μMMDV3100)for8hours.AnaliquotofcellsareharvestedforqRT-PCRofPSAandTMPRSS2mRNA.Theremainingcellsarecross-linkedusing1%paraformaldehydefor10minutes,thenglycineisaddedandsamplescentrifuged(4°C,4000rpm,5minutes)tostopfurthercrosslinking.Chromatinimmunoprecipitationisperformedusingachromatinimmunoprecipitationassaykit.ImmunoprecipitatedDNAisamplifiedbyreal-timePCR.PrimersarePSAenhancerforward-ATGTTCACATTAGTACACCTTGCCandreverse-TCTCAGATCCAGGCTTGCTTACTGTCandTMPRSS2enhancerforward-TGGTCCTGGATGATAAAAAAAGTTTandreverse-GACATACGCCCCACAACAGA^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Enzalutamideisdissolvedinvehicle(10%DMSO,45%polyethyleneglycol400,and45%saline)(Rat)^[4].

Mice^[3]
Followinga5-dayacclimationperiod,5-to9-week-oldmaleCB17SCIDmicearecastratedandallowedtorecoverforanadditional5daysbeforeinoculationwithtumorcells.LNCaPcellsco-expressingexogenousARandtheAR-dependentreporterconstructARR2-Pb-Luc(LNCaP-AR-Luxcells)areusedtogenerateaxenograftmodelofhumanprostatecancer.Beforeimplantation,LNCaP-AR-Luxcellsarepreparedbytheadditionoftrypsin-EDTA,washedwithcompletemedium,collectedandresUSPendedat20×10⁶cells/mL.CellsuspensionsaredilutedwithMatrigelto2×10⁶cells/0.2mLanddeliveredsubcutaneouslyinthesuprascapularregion.Tumorgrowthismonitoredtothevolumeof100mm³whentreatmentbegins(80days).TheobservedrateoftumortakewithLNCaP-AR-Luxcellsisbetween70%and80%.Bodyweightandtumorvolumes(width²×length/2)aremeasuredtwotothreetimesperweekwithadigitalcaliper,andtheaveragetumorvolumesaredetermined.TestdrugsaredilutedinTween80:PEG400,andstoredat4°Cuntiladministrationbyoralgavage.Eachgroupofmice(n=7)istreateddailyfor28consecutivedayswith1,10,or50mg/kgEnzalutamide,vehiclecontrol,or50mg/kgBicalutamide.Attheendofthetreatmentperiodorwhentumorvolumeexceeded1,000mm³,animalsareeuthanizedandbloodandtissuesamplesarecollectedforanalysis.
Rat^[4]
MaleSDrats(n=3)areadministeredEnzalutamidethroughthetailvein(intravenous)andbyoralgavageat1mg/kgandarekeptinmetaboliccagesafterdosing.Urineandfecessamplesarecollectedoverthefollowingtimeintervalsafterdosing:0-2,2-4,4-6,6-10,10-24,24-48,and48-72h.Themetaboliccagesarerinsedwithdistilledwater,andresiduesareaddedtotheurinesamplesat72h.ToextracttheEnzalutamidepresentinthefeces,samplesareshakenvigorouslyfor12hwith50%methanol.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].TranC,etal.Developmentofasecond-generationantiandrogenfortreatmentofadvancedprostatecancer.Science,2009,324(5928),787-790.

  [2].ScherHI,etal.AntitumouractivityofMDV3100incastration-resistantprostatecancer:aphase1-2study.Lancet,2010,375(9724),1437-1446.

  [3].GuerreroJ,etal.Enzalutamide,anandrogenreceptorsignalinginhibitor,inducestumorregressioninamousemodelofcastration-resistantprostatecancer.Prostate.2013Sep;73(12):1291-305.

  [4].KimTH,etal.Pharmacokineticsofenzalutamide,ananti-prostatecancerdrug,inrats.ArchPharmRes.2015Nov;38(11):2076-82.

464.44

C₂₁H₁₆F₄N₄O₂S

915087-33-1

RoomtemperatureincontinentalUS;mayvaryelsewhere

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.18%

SelectBatch:HY-70002-06846HY-70002-13663HY-70002-12916

DataSheet(125KB)SDS(405KB)

COA(95KB)HNMR(189KB)LCMS(145KB)

HandlingInstructions(1252KB)

• [1].TranC,etal.Developmentofasecond-generationantiandrogenfortreatmentofadvancedprostatecancer.Science,2009,324(5928),787-790.

  [2].ScherHI,etal.AntitumouractivityofMDV3100incastration-resistantprostatecancer:aphase1-2study.Lancet,2010,375(9724),1437-1446.

  [3].GuerreroJ,etal.Enzalutamide,anandrogenreceptorsignalinginhibitor,inducestumorregressioninamousemodelofcastration-resistantprostatecancer.Prostate.2013Sep;73(12):1291-305.

  [4].KimTH,etal.Pharmacokineticsofenzalutamide,ananti-prostatecancerdrug,inrats.ArchPharmRes.2015Nov;38(11):2076-82.

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