PROTAC-PD-1-PD-L1-degrader-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPROTACPD-1/PD-L1degrader-1Cat.No.:HY-131183CASNo.:2447066-37-5分⼦式:C₅₉H₅₈ClN₇O₁₁分⼦量:1076.59作⽤靶点:PROTACs;PD-1/PD-L1作⽤通路:PROTAC;Immunology/Inflammation储存⽅式:-20°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:210mg/mL(195.06mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.9289mL4.6443mL9.2886mL5mM0.1858mL0.9289mL1.8577mL10mM0.0929mL0.4644mL0.9289mL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(sealedstorage,awayfrommoistureandlight)。-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:≥1.4mg/mL(1.30mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:1.4mg/mL(1.30mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性PROTACPD-1/PD-L1degrader-1，于CereblonE3配体的PD-1/PD-L1PROTAC，抑制PD-1/PD-L1相互作⽤，IC50为39.2nM。PROTACPD-1/PD-L1degrader-1可显恢复在Hep3B/OS-8/hPD-L1和CD3T细胞共培养模型中抑制的免疫⼒。PROTACPD-1/PD-L1degrader-1以溶酶体依赖性⽅式适度降低PD-L1的蛋⽩质⽔平。IC50&TargetCereblon体外研究PROTACPD-1/PD-L1degrader-1(compoundp22)reducescellsurfacePD-L1expressionformorethan14%[1].PROTACPD-1/PD-L1degrader-1(1-10μM;24hours)reducesPD-L1expressioninadose-dependentmannerby21%and35%at1μMand10μM,respectively[1].WesternBlotAnalysis[1]CellLine:MDA-MB-231cellsConcentration:1-10μMIncubationTime:24hoursResult:ReducedPD-L1expressioninadose-dependentmannerby21%and35%at1μMand10μM,respectively.REFERENCES[1].ChengB,RenY,CaoH,ChenJ.Discoveryofnovelresorcinoldiphenylether-basedPROTAC-likemoleculesasdualinhibitorsanddegradersofPD-L1.EurJMedChem.2020;199:112377.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseo