ARD-2128-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEARD-2128Cat.No.:HY-132292CASNo.:2222111-87-5分?式:C??H??ClN?O?分?量:820.37作?靶點(diǎn):PROTACs;AndrogenReceptor作?通路:PROTAC;Others儲(chǔ)存?式:-20°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(121.90mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.2190mL6.0948mL12.1896mL5mM0.2438mL1.2190mL2.4379mL10mM0.1219mL0.6095mL1.2190mL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,awayfrommoistureandlight)。-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?。BIOLOGICALACTIVITY?物活性ARD-2128?種?效的PROTAC雄激素受體(AR)降解劑。ARD-2128可有效降低AR蛋?并抑制腫瘤組織中AR調(diào)節(jié)的因，在沒有毒性跡象的情況下抑制腫瘤?長。ARD-2128作?在前列腺癌的研究上[1]。IC50&TargetIC50:4nM(VCaP),5μM(LNCaP)[1]體外研究ARD-2128ishighlypotentandeffectiveintheinhibitionofcellgrowthintheVCaPcelllineandLNCaPcell1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemElinewiththeIC50valuesof4nMand5nM,respectively[1].ARD-2128(1,10,100,and1000nM;24hours)effectivelyreducestheARproteinlevelby>50%at1nMandachievestheARdegradationof>90%at10,100,and1000nM,respectively,inVCaPcell[1].CellViabilityAssay[1]CellLine:VCaPcellConcentration:1,10,100,and1000nMIncubationTime:24hoursResult:ReducestheARproteinlevelandachievestheARdegradation.體內(nèi)研究ARD-2128(20mg/kg;p.o.;once)iseffectiveinreducingthelevelofARproteininmiceafter24hours[1].ARD-2128(10-40mg/kg;p.o.;dailyfor21days)showsantitumoractivityintheVCaPxenograftmodelinmice[1].ARD-2128(5mg/kg;p.o.)treatmentshowstheCmax,AUC0-tandt1/2valuesof1304ng/mL,22361ngh/mLand18.8hours,respectively[1].AnimalModel:SCIDmice[1]Dosage:20mg/kgAdministration:OralResult:ReducingthelevelofARproteininmiceafter24hours.AnimalModel:SCIDmice[1]Dosage:10,20,and40mg/kgAdministration:P.o.;dailyfor21daysResult:Inhibitstumorgrowthby46,69,and63%,respectively.AnimalModel:MaleICRMice[1]Dosage:5mg/kgAdministration:P.o.(PharmacokineticAnalysis)Result:TheCmax,AUC0-tandt1/2were1304ng/mL,22361ngh/mLand18.8hours,respectively.REFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].HanX,etal.StrategiestowardDiscoveryofPotentandOrallyBioavailableProteolysisTargetingChimeraDegradersofAndrogenReceptorfortheTreatmentofProstateCancer[publishedonlineaheadofprint,2021Aug25].JMedChem.2021;10.1021/acs.jmedMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic