PROTAC-B-Raf-degrader-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPROTACB-Rafdegrader1Cat.No.:HY-111758CASNo.:2364367-27-9分⼦式:C₃₆H₃₇N₅O₁₂S分⼦量:763.77作⽤靶点:PROTACs;Raf作⽤通路:PROTAC;MAPK/ERKPathway储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:25mg/mL(32.73mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.3093mL6.5465mL13.0929mL5mM0.2619mL1.3093mL2.6186mL10mM0.1309mL0.6546mL1.3093mL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(storedundernitrogen)。-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:≥2.5mg/mL(3.27mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.27mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性PROTACB-Rafdegrader1(compound2)于Cereblon配体的⼀种B-RafPROTAC。有抗肿瘤活性。IC50&TargetB-Raf体外研究TheIC50valuesofPROTACB-Rafdegrader1(compound2)towardsMCF-7,MDA-MB-231,HepG2,LO2andB16cellsare2.7μM,21.21μM,18.70μM,41.11μMand22.68μM,respectively[1].PROTACB-Rafdegrader1(5or10μM)canacceleratethedegradationofB-Rafbyrecruitingubiquitin-proteasomesystem,andfurtheraffectstheexpressionofMcl-1,adownstreamproteinofB-Raf[1].MCF-7cellsachieveanapoptosisrateof76.70%(64.00%earlyapoptosis,12.70%lateapoptosis)after24hincubationofPROTACB-Rafdegrader1withtheconcentrationof20μM[1].PROTACB-Rafdegrader1arrestscellcycleattheG2/Mphase[1].CellCytotoxicityAssay[1]CellLine:HumanMCF-7breastcancercellline,MDA-MB-231breastcancercells,humanHepG2hepatomacells,humannormalLO2livercells,B16cells.Concentration:0-200μM.IncubationTime:72hours.Result:TheIC50valuesare2.7μM,21.21μM,18.70μM,41.11μMand22.68μMinMCF-7,MDA-MB-231,HepG2,LO2andB16cells,respectively.WesternBlotAnalysis[1]CellLine:HumanMCF-7breastcancercellline.Concentration:5or10μM.IncubationTime:24hours.Result:EffectivelyinducedthedegradationofB-RafandimpactedtheexpressionofMcl-1.ApoptosisAnalysis[1]CellLine:HumanMCF-7breastcancercellline.Concentration:2.7-20μM.IncubationTime:24hours.Result:Achievedanapoptosisrateof76.70%(64.00%earlyapoptosis,12.70%lateapoptosis)after24hincubationwiththeconcentrationof20μM.CellCycleAnalysis[1]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:HumanMCF-7breastcancercellline.Concentration:20μM.IncubationTime:24hours.Result:1.94%cellswerearrestedatG1phase,8.20%atSphase,and89.86%atG2/Mphase.REFERENCES[1].ChenH,etal.Pomalidomidehybridsactasproteolysistargetingchimeras:Synthesis,anticanceractivityandB-Rafdegradation.BioorgChem.2019Mar19;87:191-199.McePdfHeightCaution:Producthasnotbeenfullyvali