Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPROTACBETDegrader-1Cat.No.:HY-103633CASNo.:2093386-22-0分?式:C??H??N??O?分?量:871.9作?靶點:PROTACs;EpigeneticReaderDomain作?通路:PROTAC;Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:≥50mg/mL(57.35mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.1469mL5.7346mL11.4692mL5mM0.2294mL1.1469mL2.2938mL10mM0.1147mL0.5735mL1.1469mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，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沉淀、析出現象，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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1.67mg/mL(1.92mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.67mg/mL(1.92mM);SuspendedsolutionBIOLOGICALACTIVITY?物活性PROTACBETDegrader-1由Cereblon配體和BET配體相連的PROTAC，能夠在低濃度下降低BRD2，BRD3和BRD4的蛋??平。IC50&TargetBET[1]體外研究PROTACBETDegrader-1(Compound9)isapotentBETdegraderbasedonPROTAC,decreasesthelevelofBRD2,BRD3,andBRD4proteinsinRS4;11cellsat3-10nM,andinhibitsthegrowthofthiscelllinewithanIC50of4.3nM,and45.5nMforMOLM-13cells[1].戶使?本產品發(fā)表的科研?獻?ACSPharmacolTranslSci.2021Feb26.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhouB,etal.DiscoveryofaSmall-MoleculeDegraderofBromodomainandExtra-Terminal(BET)ProteinswithPicomolarCellularPotenciesandCapableofAchievingTumorRegression.JMedChem.2018Jan25;61(2):462-481.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-