Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPROTACB-Rafdegrader1Cat.No.:HY-111758CASNo.:2364367-27-9分?式:C??H??N?O??S分?量:763.77作?靶點:PROTACs;Raf作?通路:PROTAC;MAPK/ERKPathway儲存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實驗DMSO:25mg/mL(32.73mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.3093mL6.5465mL13.0929mL5mM0.2619mL1.3093mL2.6186mL10mM0.1309mL0.6546mL1.3093mL請根據(jù)產(chǎn)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(fù)凍融造成的產(chǎn)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(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(xiàn)沉淀、析出現(xiàn)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:≥2.5mg/mL(3.27mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.27mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性PROTACB-Rafdegrader1(compound2)于Cereblon配體的?種B-RafPROTAC。有抗腫瘤活性。IC50&TargetB-Raf體外研究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?邊的抑制劑?師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