PROTAC-BET-Degrader-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPROTACBETDegrader-1Cat.No.:HY-103633CASNo.:2093386-22-0分⼦式:C₄₄H₄₅N₁₁O₉分⼦量:871.9作⽤靶点:PROTACs;EpigeneticReaderDomain作⽤通路:PROTAC;Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥50mg/mL(57.35mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.1469mL5.7346mL11.4692mL5mM0.2294mL1.1469mL2.2938mL10mM0.1147mL0.5735mL1.1469mL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。-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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1.67mg/mL(1.92mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.67mg/mL(1.92mM);SuspendedsolutionBIOLOGICALACTIVITY⽣物活性PROTACBETDegrader-1由Cereblon配体和BET配体相连的PROTAC，能够在低浓度下降低BRD2，BRD3和BRD4的蛋⽩⽔平。IC50&TargetBET[1]体外研究PROTACBETDegrader-1(Compound9)isapotentBETdegraderbasedonPROTAC,decreasesthelevelofBRD2,BRD3,andBRD4proteinsinRS4;11cellsat3-10nM,andinhibitsthegrowthofthiscelllinewithanIC50of4.3nM,and45.5nMforMOLM-13cells[1].户使⽤本产品发表的科研⽂献•ACSPharmacolTranslSci.2021Feb26.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhouB,etal.DiscoveryofaSmall-MoleculeDegraderofBromodomainandExtra-Terminal(BET)ProteinswithPicomolarCellularPotenciesandCapableofAchievingTumorRegression.JMedChem.2018Jan25;61(2):462-481.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-