FT671-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFT671Cat.No.:HY-107985CASNo.:1959551-26-8分⼦式:C₂₄H₂₃F₄N₇O₃分⼦量:533.48作⽤靶点:Deubiquitinase作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(93.72mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8745mL9.3724mL18.7448mL5mM0.3749mL1.8745mL3.7490mL10mM0.1874mL0.9372mL1.8745mL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:≥5mg/mL(9.37mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(9.37mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(9.37mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性FT671有效、⾮共价的、选择性的USP7抑制剂，IC50值为52nM，与USP7催化域结合的Kd值为65nM。IC50&TargetIC50:52nM(USP7)[1]Kd:65nM(USP7)[1]体外研究FT671increasesp53proteinlevelsinHCT116orboneosteosarcoma(U2OS)celllines,leadingtoinductionofp53targetgenesincludingBBC3(whichencodesPUMA),CDKN1A(p21),RPS27L(S27L)andMDM2.FT671leadstothedegradationofN-Mycandupregulationofp53intheneuroblastomacelllineIMR-32.FT671alsostabilizesp53intheMM.1Smultiplemyelomacellline,whichcorrelateswithincreasedMDM2ubiquitinationandleadstoexpressionofp53targetgenes[1].体内研究FT671(100mg/kgand200mg/kg,Oralgavage,daily)treatmentinmiceleadstoasignificantdose-dependentinhibitionoftumorgrowth.AndFT671iswell-torelatedevenathighdoses[1].AnimalModel:Non-obesediabetic-severecombinedimmunodeficient(NOD–SCID)miceimplantedwithMM.1Scells[1].Dosage:100mg/kgand200mg/kg.Administration:Oralgavagedaily.Result:Ledtoasignificantdose-dependentinhibitionoftumorgrowth.户使⽤本产品发表的科研⽂献•CellRep.2021Oct12;37(2):109819.•LeidenUiversity.FacultyofMedicine,LeidenUniversityMedicalCenter.2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TurnbullAP,etal.MolecularbasisofUSP7inhibitionbyselectivesmall-moleculeinhibitors.Nature.2017Oct26;550(7677):481-486.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.