A1874-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEA1874Cat.No.:HY-114305CASNo.:2064292-12-0分?式:C??H??Cl?F?N?O?S分?量:1173.59作?靶點:PROTACs;EpigeneticReaderDomain作?通路:PROTAC;Epigenetics儲存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實驗DMSO:150mg/mL(127.81mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM0.8521mL4.2604mL8.5209mL5mM0.1704mL0.8521mL1.7042mL10mM0.0852mL0.4260mL0.8521mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(2.13mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(2.13mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性A1874?種以nutlin（MDM2配體）為礎(chǔ)的、BRD4-降解的PROTAC，DC50值為32nM(誘導(dǎo)細胞內(nèi)的BRD4降解)。有效抑制多種癌細胞增殖[1]。IC50&TargetBRD4體外研究TreatmentofHCT116cellsofA1874(0-10μM,24hours)inducesadose-dependentknockdownofBRD4levels,withnear-maximumknockdownby100nmol/Landamaximumdegradation(Dmax)ofBRD4of98%ofthelevelsincontrol(0.1%DMSO-treated)cells[1].TreatmentofHCT116cellsofA1874(0-10μM,24hours)increasesp53levelsintheHCT116cellsandshoweddose-dependentp53stabilization[1].WesternBlotAnalysis[1]CellLine:HCT116cells.Concentration:0-10μM.IncubationTime:24hours.Result:InducedadosedependentknockdownofBRD4levels,withnear-maximumknockdownby100nM.Increasedp53levelsandshoweddose-dependentp53stabilization.REFERENCES[1].HinesJ,etal.MDM2-RecruitingPROTACOffersSuperior,SynergisticAntiproliferativeActivityviaSimultaneousDegradationofBRD4andStabilizationofp53.CancerRes.2019Jan1;79(1):251-262.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly