MBQ-167-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMBQ-167Cat.No.:HY-112842CASNo.:2097938-73-1分⼦式:C₂₂H₁₈N₄分⼦量:338.41作⽤靶点:Ras;CDK作⽤通路:GPCR/GProtein;CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:155mg/mL(458.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9550mL14.7750mL29.5500mL5mM0.5910mL2.9550mL5.9100mL10mM0.2955mL1.4775mL2.9550mL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。-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:≥2.58mg/mL(7.62mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:2.58mg/mL(7.62mM);Clearsolution;NeedwarmingBIOLOGICALACTIVITY⽣物活性MBQ-167Ras相关的C3型⾁毒素底物(Rac)和细胞分裂周期蛋⽩(Cdc42)的双抑制剂，其对Rac1/2/3的IC50值为103nM，对Cdc42的IC50值为78nM。IC50&TargetCdc42Ras1/2/378nM(IC50)103nM(IC50)体外研究MBQ-167(≥100nM)inducesalossofpolarityinmetastaticbreastcancercells.Treatmentwith500nMMBQ-167for24hresultsin~95%cellroundinganddetachmentfromthesubstratuminmetastaticMDA-MB-231cells.Moreover,MBQ-167inducesthisphenotypeinmultiplemesenchymalcancercelltypesincludingGFP-HER2-BM,MDA-MB-468,andHs578thumanbreastcancercells,aswellasMia-PaCa-2pancreaticcancercells,SKOV3ovariancancercells,AGSandNCI-N87gastriccancercells,andSH-SY5Yneuroblastomacells.Followingtreatmentwith250nMMBQ-167for24h,theattachedpopulationofMDA-MB-231cellsdemonstratea~25%decreaseinRacactivationwhilethedetachedcellsaremoreresponsivewitha~75%decrease.Atearliertimes(6h),treatmentwith250or500nMMBQ-167,induceainhibitioninRacactivityintheattachedcellpopulation,whilethedetachedpopulationdemonstratea~40-50%inhibition[1].体内研究MBQ-167-treatedmicedemonstrateastatisticallysignificantreductionintumorgrowth.Atsacrifice,1.0mg/kgBWofMBQ-167resultsina~80%reductionintumorgrowth,andthe10mg/kgBWMBQ-167treatmentresultsin~95%reductionintumorgrowth.SinceEHop-016onlyexerts~40%reductionoftumorgrowthat10mg/kgBW,MBQ-167is10XmoreeffectivethanEHop-016.MBQ-167treatedmicedemonstratesimilardoublingtimesforbothtreatments(10and11days)[1].PROTOCOLAnimalMice[1]Administration[1]Femaleathymicnu/numice,4to5wkoldareused.GFP-HER2-BMcells(~5×105)inMatrigelareinjectedatthefourthrightmammaryfatpadunderisofluoraneinhalationtoproduceorthotopicprimarytumors.Aftertumorestablishment(1wkpost-inoculation),animalsarerandomlydividedintotreatmentgroups(n=6).Micearetreatedwithvehicle(12.5%ethanol,12.5%Cremophor,and75%1XPBSpH7.4),or1or10mg/kgBWMBQ-167byi.p.injectionina100μLvolume3Xawk.Treatmentscontinueuntilsacrificeatday65[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Nature.2022Oct;610(7931):366-372.•ClinTranslMed.2022Jun;12(6):e850.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].Humphries-BickleyT,etal.CharacterizationofaDualRac/Cdc42InhibitorMBQ-167inMetastaticCancer.MolCancerTher.2017May;16(5):805-818.McePdfHeightCaution:Produ