Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEXZ739Cat.No.:HY-133557CASNo.:2365172-19-4分?式:C??H??ClF?N?O??S?分?量:1349.99作?靶點:PROTACs;Bcl-2Family;Apoptosis作?通路:PROTAC;Apoptosis儲存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數據體外實驗DMSO:20mg/mL(14.81mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM0.7407mL3.7037mL7.4075mL5mM0.1481mL0.7407mL1.4815mL10mM0.0741mL0.3704mL0.7407mL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(storedundernitrogen)。-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%salineSolubility:2mg/mL(1.48mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性XZ739?種于Cereblon的PROTACBCL-XL(Bcl-2家族成員)降解劑，作?于MOLT-4細胞，處理16?時后，DC50值為2.5nM[1]。XZ739還通過caspase介導的凋亡(apoptosis)誘導細胞死亡[1]。IC50&TargetBcl-xLCereblon2.5nM(DC50)體外研究XZ739(0.001-10μM;48hours)potentlyreducestheviabilityofT-ALLMOLT-4,B-ALLRS4;11,SCLCNCI-H146cells,andplateletsafter48htreatmentwithIC50sof10.1,41.8,25.3,and1217nM,respectively.XZ739has>100-foldselectivityforMOLT-4cellsoverhumanplatelets[1].XZ739(1.2-300nM;16hours)inducesBCL-XLdegradationinMOLT-4cells[1].TheBCL-XLdegradationinducedbyXZ739inMOLT-4israpid,startingwithin2h;and8hafterXZ739treatment,morethan96%oftheBCL-XLisdegradedwith100nMofXZ739[1].CellViabilityAssay[1]CellLine:HumanplateletsandMOLT-4cellsConcentration:0.001,0.01,0.1,1,and10μMIncubationTime:48hoursResult:IC50valueswere10.1nMand1217nMforMOLT-4cellsandplatelets,respectively.WesternBlotAnalysis[1]CellLine:MOLT-4cellsConcentration:1.2,3.7,11,33,100,300nMIncubationTime:16hoursResult:Dose-dependentlyinducedBCL-XLdegradation.REFERENCES[1].XuanZhang,etal.DiscoveryofPROTACBCL-XLDegradersasPotentAnticancerAgentsWithLowOn-TargetPlateletToxicity.EurJMedChem.2020Apr15;192:112186.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese