PROTAC-BRD4-Degrader-8-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPROTACBRD4Degrader-8Cat.No.:HY-138555分⼦式:C₅₃H₆₁F₂N₉O₁₁S₂分⼦量:1102.23作⽤靶点:PROTACs;EpigeneticReaderDomain作⽤通路:PROTAC;Epigenetics储存⽅式:-20°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:90mg/mL(81.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.9073mL4.5363mL9.0725mL5mM0.1815mL0.9073mL1.8145mL10mM0.0907mL0.4536mL0.9073mL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(protectfromlight)。-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:≥4.5mg/mL(4.08mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥4.5mg/mL(4.08mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性PROTACBRD4Degrader-8⼀种由vonHippel-Lindau配体和BRD4配体相连的PROTAC，对BRD4BD1和BD2的IC50值分别为1.1nM和1.4nM。PROTACBRD4Degrader-8能够有效降解PC3前列腺癌细胞中的BRD4蛋⽩。IC50&TargetIC50:1.1nM(BRD4BD1),1.4nM(BRD4BD2)[1]体外研究PROTACBRD4Degrader-8(compound8;6days)inhibitstheproliferationofPC3prostatecancercells,withanIC50of28nM[1].PROTACBRD4Degrader-8(4h)suppressesMYCgenetranscriptinMV4-11AMLcells,withanIC50of11nM[1].PROTACBRD4Degrader-8(4h)potentlydegradestheBRD4proteininPC3prostatecancercells,withanDC50of7.5nM[1].REFERENCES[1].DragovichPS,et,al.Antibody-MediatedDeliveryofChimericBRD4Degraders.Part2:ImprovementofInVitroAntiproliferationActivityandInVivoAntitumorEfficacy.JMedChem.2021Mar11;64(5):2576-2607.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400