Elacestrant-RAD1901-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEElacestrantCat.No.:HY-19822CASNo.:722533-56-4Synonyms:RAD1901分⼦式:C₃₀H₃₈N₂O₂分⼦量:458.63作⽤靶点:EstrogenReceptor/ERR作⽤通路:Others储存⽅式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:160mg/mL(348.87mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1804mL10.9020mL21.8041mL5mM0.4361mL2.1804mL4.3608mL10mM0.2180mL1.0902mL2.1804mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥4mg/mL(8.72mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥4mg/mL(8.72mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥4mg/mL(8.72mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Elacestrant(RAD1901)⼀种具有⼝服活性的的选择性雌激素受体(ER)降解剂(SERD)，对ERα和ERβ的IC50值分别为48和870nM。IC50&TargetIC50:48nM(ERα),870nM(ERβ)[1]体外研究RAD1901selectivelybindstoanddegradestheERandisapotentantagonistofER-positivebreastcancercellproliferation.RAD1901treatmentexhibitsdose-dependentinhibitionofERαexpression,withanEC50of0.6nM.TreatmentofER-positiveMCF-7cellswithE2resultsinapotentanddose-dependentincreaseinproliferation,withanEC50of4pM.TreatmentofcellswithRAD1901inthepresenceof10pME2resultsinadose-dependentdecreaseinproliferation,withanIC50valueof4.2nM[1].体内研究RAD1901producesarobustandprofoundinhibitionoftumorgrowthinMCF-7xenograftmodels.RAD1901-treatedanimalssurvivedlongerthanthosetreatedwitheithercontrolorfulvestrant.RAD1901preservesovariectomy-inducedbonelossandpreventestheuterotropiceffectsofE2[1].PROTOCOLKinaseAssay[1]RAD1901isseriallydilutedinES2screeningbuffertoconcentrationsrangingfrom10to10-6μM.Aliquots(25μL)ofeachdilutionareaddedtoablack384-wellmicrotiterplate,intriplicate.TheER–Fluormonecomplexispreparedasdirected,with2nMFluormoneES2and30nMER.A25μLaliquotofthispreparationisaddedtoeachreactionwell.Theplatesaresealedandincubatedinthedarkatroomtemperaturefor4h.Polarizationvaluesforeachwellaremeasuredandplottedagainsttheconcentrationofthetestcompound.TheIC50isdeterminedfromatleastthreeindependentexperiments,withE2servingasapositivecontrol[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[1]Forproliferationassays,MCF-7cellsaretreatedwith2%charcoal-strippedFBS–MEMcontaining10pME2witheitherRAD1901oradditionalE2atconcentrationsrangingfrom10-9to1M.Themediumisremovedafter48hofincubationandthecellsarelysedbyadding100μlofCellTiterGlo.Theplatesaregentlymixedonaplateshakerfor10minbeforetheluminescentsignalismeasuredonaluminometer.TheEC50andIC50ofthetestcompoundarethendefined[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:RAD1901isstoredasadrypowder,formulatedforuseasahomogenoussuspensionin0.5%(w/v)Administration[1]methylcelluloseindeionizedwater.Fourteendaysaftertumorcellimplantation,themicearerandomizedinto2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEninegroupsof15animalseachandtreatedwithvehicle,tamoxifen(1mg/animaleveryotherday),fulvestrant(0.5mg/animaldaily),orRAD1901(0.3,1,3,10,30,60,90,and120mg/kgdaily).Tumorvolumesareevaluatedtwiceperweek[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•JMedChem.2020Oct8;63(19):11085-11099.•MolCancerTher.2020Jul;19(7):1395-1405.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GarnerF,etal.RAD1901:anovel,orallybioavailableselectiveestrogenreceptordegraderthatdemonstratesantitumoractivityinbreastcancerxenograftmodels.AnticancerDrugs.201