FT671-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFT671Cat.No.:HY-107985CASNo.:1959551-26-8分?式:C??H??F?N?O?分?量:533.48作?靶點:Deubiquitinase作?通路:CellCycle/DNADamage儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(93.72mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8745mL9.3724mL18.7448mL5mM0.3749mL1.8745mL3.7490mL10mM0.1874mL0.9372mL1.8745mL請根據(jù)產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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:≥5mg/mL(9.37mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(9.37mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(9.37mM);ClearsolutionBIOLOGICALACTIVITY?物活性FT671有效、?共價的、選擇性的USP7抑制劑，IC50值為52nM，與USP7催化域結合的Kd值為65nM。IC50&TargetIC50:52nM(USP7)[1]Kd:65nM(USP7)[1]體外研究FT671increasesp53proteinlevelsinHCT116orboneosteosarcoma(U2OS)celllines,leadingtoinductionofp53targetgenesincludingBBC3(whichencodesPUMA),CDKN1A(p21),RPS27L(S27L)andMDM2.FT671leadstothedegradationofN-Mycandupregulationofp53intheneuroblastomacelllineIMR-32.FT671alsostabilizesp53intheMM.1Smultiplemyelomacellline,whichcorrelateswithincreasedMDM2ubiquitinationandleadstoexpressionofp53targetgenes[1].體內研究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.戶使?本產品發(fā)表的科研?獻?CellRep.2021Oct12;37(2):109819.?LeidenUiversity.FacultyofMedicine,LeidenUniversityMedicalCenter.2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TurnbullAP,etal.MolecularbasisofUSP7inhibitionbyselectivesmall-moleculeinhibitors.Nature.2017Oct26;550(7677):481-486.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.