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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Enzalutamide(Synonyms: MDV3100)/HY-70002/5mg
商品详细Medchemexpress/Enzalutamide(Synonyms: MDV3100)/HY-70002/5mg
Medchemexpress/Enzalutamide(Synonyms: MDV3100)/HY-70002/5mg
Medchemexpress/Enzalutamide(Synonyms: MDV3100)/HY-70002/5mg
商品编号： HY-70002-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1100.00
美元价： 660.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
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商品介绍
Enzalutamideisanandrogen-receptor(AR)antagoNISTwithIC50of36nMinLNCaPcells.

CustomerValidation

  • •CancerDiscov.2017Jan;7(1):54-71.
  • •ClinCancerRes.2017Sep12.pii:clincanres.0901.2017.
  • •ClinCancerRes.2015Nov1;21(21):4845-55.
  • •ClinCancerRes.2015Apr1;21(7):1675-87.
  • •ClinCancerRes.2014Dec15;20(24):6367-78.
  • •CancerRes.2016Nov15;76(22):6701-6711.
  • •CancerRes.2013Aug15;73(16):5206-17.
  • •Oncogene.2014Jun12;33(24):3140-50.
  • •Nanoscale.2017Jul13;9(27):9676-9684.
  • •CellDeathDis.2014Jul17;5:e1338.
  • •MolCancerTher.2017Oct;16(10):2281-2291.
  • •MolCancerTher.2016Sep;15(9):2107-18.
  • •MolCancerTher.2015Mar;14(3):713-26.
  • •MolCancerTher.2013May;12(5):567-76.
  • •Oncotarget.2016Sep13;7(37):59781-59794.
  • •Oncotarget.2016Jun28;7(26):40690-40703.
  • •Oncotarget.2015Aug21;6(24):20474-84.
  • •Oncotarget.2014Oct15;5(19):9007-21.
  • •MolCancerRes.2016Jun;14(6):574-85.
  • •JSteroidBiochemMolBiol.2014Oct;144PtB:436-44.
  • •SciRep.2017Jun8;7(1):3058.
  • •SciRep.2016Sep28;6:33968.
  • •Prostate.2017Feb;77(3):309-320.
  • •Prostate.2016Sep;76(13):1192-202.
  • •HormCancer.2017Aug;8(4):243-256.
  • •IntJMolSci.2016Sep1;17(9).pii:E1458.
  • •IntJOncol.2017Jan;50(1):75-84.
  • •DigDisSci.2017Oct20.
  • •PLoSOne.2016Apr5;11(4):e0152861.
  • •UniversityofBritishColumbia.2017-04-18.
  • •Patent.US20140088178A1.
  • •Annualrept.15Sep2012-14Sep2013
Description

Enzalutamideisanandrogen-receptor(AR)antagonistwithIC50of36nMinLNCaPcells.

IC50&Target

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

InVitro

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].

InVivo

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

ClinicalTrial
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References

  • [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.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.1531mL10.7657mL21.5313mL
5mM0.4306mL2.1531mL4.3063mL
10mM0.2153mL1.0766mL2.1531mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

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.

AnimalAdministration
[3][4]

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.

References

  • [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.

MolecularWeight

464.44

Formula

C₂₁H₁₆F₄N₄O₂S

CASNo.

915087-33-1

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:99.18%