A1874-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEA1874Cat.No.:HY-114305CASNo.:2064292-12-0分⼦式:C₅₈H₆₂Cl₃F₂N₉O₇S分⼦量:1173.59作⽤靶点:PROTACs;EpigeneticReaderDomain作⽤通路:PROTAC;Epigenetics储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:150mg/mL(127.81mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.8521mL4.2604mL8.5209mL5mM0.1704mL0.8521mL1.7042mL10mM0.0852mL0.4260mL0.8521mL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(storedundernitrogen)。-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:≥2.5mg/mL(2.13mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(2.13mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性A1874⼀种以nutlin（MDM2配体）为础的、BRD4-降解的PROTAC，DC50值为32nM(诱导细胞内的BRD4降解)。有效抑制多种癌细胞增殖[1]。IC50&TargetBRD4体外研究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