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Medchemexpress/Mifepristone(Synonyms: RU486; RU 38486)/HY-13683/500mg
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Medchemexpress/Mifepristone(Synonyms: RU486; RU 38486)/HY-13683/500mg
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MedChemExp
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HY-13683-10mM*1mLinDMSO
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Mifepristoneisaprogesteronereceptor(PR)antagoNIST(IC50=0.2nM)inaT47Dcell-basedassay,alsoisaglucocorticoidreceptor(GR)antagonist(IC50=2.6nM)inanA549cell-basedassay.

CustomerValidation

  • •SciRep.2017Jul26;7(1):6501.
  • •BiochemBiophysResCommun.2017Nov23.pii:S0006-291X(17)32327-6.
  • •EvidBasedComplementAlternatMed.2016;2016:5850739.
Description

Mifepristoneisaprogesteronereceptor(PR)antagonist(IC50=0.2nM)inaT47Dcell-basedassay,alsoisaglucocorticoidreceptor(GR)antagonist(IC50=2.6nM)inanA549cell-basedassay.

IC50&Target

IC50:0.2nM(progesteronereceptor,inT47Dcells),2.6nM(glucocorticoidreceptor,inA549cells)[1]

InVitro

Thediscoveryofthefirstcompetitiveprogesteroneantagonist,Mifepristone,hasstimulatedanintensesearchformorepotentandmoreselectiveantiprogestins[1].Cellgrowthisevaluatedafter4daysofexposuretoMifepristoneat10μM,aconcentrationclosetotheplasmaconcentrationachievableinhumans.TheantiproliferativeeffectofCisplatinispotentiatedwhenadministeredincombinationwithMifepristoneinHeLacells.TheIC50ofCisplatinincombinationwithMifepristoneislower(14.2μM)thanthatofCisplatinalone(34.2μM)inHeLacellswithanapproximately2.5-folddifference.AftertreatmentwithMifepristone,theaccumulationofintracellularCisplatininHeLacellsis2-foldgreater,representingasignificantdifference(p=0.009),comparewithCisplatinalonefrom0.79to1.52μg/mgofprotein[2].

InVivo

ThecervixtumorxenograftmodelsaretreatedwithCisplatinalone,thereisatumorgrowthinhibitioncomparewithcontrolgroup.However,thetumorweightlossisevenmoresignificant(p<0.05) with="" the="" combination="" of="" cisplatin="" and="" mifepristone="" at="" the="" doses="" used,="" showing="" a="" decrease="" of="" ~50%="" compared="" with="" the="" treatments="" alone="" by="" the="" end="" of="" the="">[2].AdultmaleSprague-Dawleyratsaresubjectedtoa4-daybinge-likeEtOHadministrationregimen(3to5g/kg/i.g.every8hoursdesignedtoproducepeakbloodEtOHlevels(BELs)of<300 mg/dl).="" subgroups="" of="" animals="" receive="" s.c.="" injection="" of="" mifepristone="" (20="" or="" 40="" mg/kg="" in="" peanut="" oil).="" although="" mifepristone="" produces="" no="" significant="" changes="" in="" behavior="" of="" etoh-naïve="" animals,="" pretreatment="" with="" mifepristone="" (40="" mg/kg)="" significantly="" reducesthe="" severity="" of="" etoh="" withdrawal.="" asignificant="" interaction="" between="" diet="" and="" drug,="" f(5,55)="3.92,"><0.05, such="" that="" etoh-treated="" animals="" receiving="" vehicle="" or="" 20="" mg/kg="" of="" mifepristone="" displayssignificantly="" more="" signs="" of="" etoh="" withdrawal="" than="" does="" etoh-naïve="" animals="" receiving="" the="" same="" drug="" treatment.="" importantly,="" treatment="" with="" 40="" mg/kg="" of="" mifepristone="" significantly="" reduces="" the="" severity="" of="" etoh="" withdrawal,="" in="" a="" dose-dependent="">[3].

ClinicalTrial
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References

  • [1].JiangW,etal.Newprogesteronereceptorantagonists:phosphorus-containing11beta-aryl-substitutedsteroids.BioorgMedChem.2006Oct1;14(19):6726-32.

    [2].JuradoR,etal.Cisplatincytotoxicityisincreasedbymifepristoneincervicalcarcinoma:aninvitroandinvivostudy.OncolRep.2009Nov;22(5):1237-45.

    [3].Sharrett-FieldL,etal.MifepristonePretreatmentReducesEthanolWithdrawalSeverityInVivo.AlcoholClinExpRes.2013Aug;37(8):1417-23.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.3278mL11.6390mL23.2780mL
5mM0.4656mL2.3278mL4.6556mL
10mM0.2328mL1.1639mL2.3278mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[1]

T47Dhumanbreastcancercellsareplatedin96-welltissuecultureplatesat10,000cellsperwellinassaymedium[RPMImediumwithoutphenolredcontaining5%(v/v)charcoal-treatedFBSand1%(v/v)penicillin-streptomycin].Twodayslater,themediumisdecantedandMifepristoneorcontrolisaddedatafinalconcentrationof0.1%(v/v)dimethylsulfoxideinfreshassaymedium.Twenty-fourhourslater,analkalinephosphataseassayisperformedusingaSEAPkit.Briefly,themediumisdecantedandthecellsarefixedfor30minatroomtemperaturewith5%(v/v)formalin.ThecellsarewashedonceatroomtemperaturewithHanks’bufferedsalinesolution.Equalvolumes(0.05mL)of1×dilutionbuffer,assaybuffer,and1:20substrate/enhancermixturearethenadded.Aftera1-hincubationatroomtemperatureinthedark,thelysateistransferredtoawhite96-wellplateandluminescenceisreadusingaLuminoSkanAscent[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[2]

Mifepristoneisreconstitutedinabsoluteethanolandstored(-20˚C),andthendilutedwithappropriatemediabeforeuse[2].

TheHeLaandCaSkihumancervicalcancercelllinesareused.TheeffectofMifepristoneonproliferationofcellsexposedtoCisplatinisevaluatedusingtheXTTassay.TheassayisbasedonthecleavageoftheyellowtetrazoliumsaltXTTtoformanorangeformazandyebymetabolicallyactivecells.Theprocedureisasfollows.Cellsareseededinto96-wellplates;Costaratadensityof6×103viablecellsperwellin100μLculturemedium.AttheendoftreatmentwithCisplatinaloneorthecombinationofCisplatinplusMifepristone,50μLXTTisaddedtoeachwell(finalconcentration0.3mg/mL),followbyincubationfor4hinahumidifiedatmospherecontaining5%CO2at37˚C.Theabsorbanceofthesamplesismeasuredspectrophotometricallyat492nmusingamicrotiterplateELISAreader[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[2][3]

MifepristoneissUSPendedinpeanutoil(Rat)[3].

Mice[2]
FemaleNudemicebetween6-8weeksofageareimplantedsubcutaneouslywith6×106HeLacellsinaflank.Oncetumorsare~5×5mm,theanimalsarepair-matchedintotreatmentandcontrolgroups.Eachgroupconsistof8tumor-bearingmice.Theintraperitonealadministrationofdrugsorvehiclebeginonday0.Cisplatin,asasingleagent,isadministeredintraperitoneallyatadoseof3mg/kgdailyondays1through3;thedoseofMifepristone,asasingleagent,is2mg/kg/daysubcutaneouslyfor3days;inthecombinationstudy,themiceconcurrentlyreceiveCisplatinonthesameschedule,andMifepristoneatthesamedose3daysprevioustotheadministrationofCisplatin.Thecontrolanimalsreceiveonlythevehicle.Afteradministrationofthedrugs,miceareweighedandthetumorsaremeasuredwithacalipertwiceweekly.Thetumorweightiscalculated.Experimentisconductedfor74days,afterwhichtimeallanimalsareweighedandhumanelyeuthanized.
Rat[3]
AdultmaleSprague-Dawleyrats,weighingbetween224and245guponarrival,areused.Mifepristone(20or40mg/kg)orvehicle(peanutoil)areadministeredsubcutaneously(s.c.)oncedailyfollowingthe0800administrationofEtOHorcontroldiet.Mifepristoneissuspendedinpeanutoilandsonicatedfor30minutesatleast24hourspriortoinjection,itisthenstoredat4°Cuntilneeded.Suspensionisvortexedfor10to15minutespriortoandasneededthroughoutdosing.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].JiangW,etal.Newprogesteronereceptorantagonists:phosphorus-containing11beta-aryl-substitutedsteroids.BioorgMedChem.2006Oct1;14(19):6726-32.

    [2].JuradoR,etal.Cisplatincytotoxicityisincreasedbymifepristoneincervicalcarcinoma:aninvitroandinvivostudy.OncolRep.2009Nov;22(5):1237-45.

    [3].Sharrett-FieldL,etal.MifepristonePretreatmentReducesEthanolWithdrawalSeverityInVivo.AlcoholClinExpRes.2013Aug;37(8):1417-23.

MolecularWeight

429.59

Formula

C₂₉H₃₅NO₂

CASNo.

84371-65-3

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥59mg/mL

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

Purity:98.17%

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