Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEElacestrantdihydrochlorideCat.No.:HY-19822ACASNo.:1349723-93-8Synonyms:RAD1901dihydrochloride分?式:C??H??Cl?N?O?分?量:531.56作?靶點(diǎn):EstrogenReceptor/ERR作?通路:Others儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(188.13mM;Needultrasonic)H2O:50mg/mL(94.06mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8813mL9.4063mL18.8126mL5mM0.3763mL1.8813mL3.7625mL10mM0.1881mL0.9406mL1.8813mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：1%DMSO>>99%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥0.57mg/mL(1.07mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.70mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.70mM);Clearsolution4.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.70mM);Clearsolution5.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.87mg/mL(5.40mM);Clearsolution6.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.87mg/mL(5.40mM);ClearsolutionBIOLOGICALACTIVITY?物活性Elacestrantdihydrochloride(RAD1901dihydrochloride)?種具有?服活性的的選擇性雌激素受體(ER)降解劑(SERD)，對(duì)ERα和ERβ的IC50值分別為48和870nM。IC50&TargetIC50:48nM(ERα),870nM(ERβ)[1]體外研究RAD1901selectivelybindstoanddegradestheERandisapotentantagonistofER-positivebreastcancercellproliferation.RAD1901treatmentexhibitsdose-dependentinhibitionofERαexpression,withanEC50of0.6nM.TreatmentofER-positiveMCF-7cellswithE2resultsinapotentanddose-dependentincreaseinproliferation,withanEC50of4pM.TreatmentofcellswithRAD1901inthepresenceof10pME2resultsinadose-dependentdecreaseinproliferation,withanIC50valueof4.2nM[1].體內(nèi)研究RAD1901producesarobustandprofoundinhibitionoftumorgrowthinMCF-7xenograftmodels.RAD1901-treatedanimalssurvivedlongerthanthosetreatedwitheithercontrolorICI182780.RAD1901preservesovariectomy-inducedbonelossandpreventestheuterotropiceffectsofE2[1].PROTOCOLCellAssay[1]Forproliferationassays,MCF-7cellsaretreatedwith2%charcoal-strippedFBS–MEMcontaining10pME2witheitherRAD1901oradditionalE2atconcentrationsrangingfrom10-9to1M.Themediumisremovedafter48hofincubationandthecellsarelysedbyadding100μlofCellTiterGlo.Theplatesaregentlymixedonaplateshakerfor10minbeforetheluminescentsignalismeasuredonaluminometer.TheEC50andIC50ofthetestcompoundarethendefined[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:RAD1901isstoredasadrypowder,formulatedforuseasahomogenoussuspensionin0.5%(w/v)Administration[1]methylcelluloseindeionizedwater.Fourteendaysaftertumorcellimplantation,themicearerandomizedintoninegroupsof15animalseachandtreatedwithvehicle,CI47699(1mg/animaleveryotherday),ICI182780(0.5mg/animaldaily),orRAD1901(0.3,1,3,10,30,60,90,and120mg/kgdaily).Tumorvolumesare2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEevaluatedtwiceperweek[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JMedChem.2020Oct8;63(19):11085-11099.?MolCancerTher.2020Jul;19(7):1395-1405.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GarnerF,etal.RAD1901:anovel,orallybioavailableselectiveestrogenreceptordegraderthatdemonstratesantitumoractivityinbreastcancerxenograftmodels.AnticancerDrugs.2015Oct;26(9):948-56.