EC359-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEC359Cat.No.:HY-120142CASNo.:2012591-09-0分?式:C??H??F?O?分?量:540.68作?靶點:Apoptosis作?通路:Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(231.19mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8495mL9.2476mL18.4952mL5mM0.3699mL1.8495mL3.6990mL10mM0.1850mL0.9248mL1.8495mL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。-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:≥2.08mg/mL(3.85mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.85mM);ClearsolutionBIOLOGICALACTIVITY?物活性EC359?種有效的，選擇性的，?親和?的和?服的?物利?度??病抑制因?受體(LIFR)抑制劑，其Kd值為10.2nM，可直接與LIFR相互作?以有效阻斷LIF/LIFR相互作?。IC50&TargetKd:10.2nM(leukemiainhibitoryfactorreceptor)[1]體外研究EC359(0-100nM;3days;BT-549,SUM-159,MDA-MB-231,MDA-MB-468,andHCC1806cells)treatmentreducescellviabilityinadose-dependentmanner[1].EC359(20nM,25nM;72hours;MDA-MB-231andBT-549cells)treatmentsignificantlyincreasescaspase-3/7activityandAnnexinV-positivecellsinbothMDAMB-231andBT-549cells.EC359exhibitssignificantinhibitoryactivityoninvasionandpromotesapoptosisofTNBCcells[1].EC359(100nM;12hours;BT549cells)treatmentsignificantlyreducestheexpressionofseveral(suchasSTAT1TGFB1,JUNB,MCL-1,etc)knownSTAT3targetgenes[1].EC359(100nM;1hour;MDA-MB-231andBT-549cells)treatmentsubstantiallyreducestheLIFactivationofSTAT3,alsoreducestheSTAT3activationbyOSMandCNTF.EC359treatmentsubstantiallydecreasesthephosphorylationofAKT,mTOR,S6,andERK1/2inMDA-MB231andBT-549cells.EC359treatmentalsoincreasesthephosphorylationofproapoptoticp38MAPKinBT549cells[1].CellViabilityAssay[1]CellLine:BT-549,SUM-159,MDA-MB-231,MDA-MB-468,andHCC1806cellsConcentration:0nM,1.5nM,12.5nM,25nM,50nM,100nMIncubationTime:3daysResult:Reducedcellviabilityinadose-dependentmanner.ApoptosisAnalysis[1]CellLine:MDA-MB-231andBT-549cellsConcentration:20nM,25nMIncubationTime:72hoursResult:PromotedapoptosisofTNBCcells.RT-PCR[1]CellLine:BT549cellsConcentration:100nM2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:12hoursResult:ReducedtheexpressionofseveralknownSTAT3targetgenes.WesternBlotAnalysis[1]CellLine:MDA-MB-231andBT-549cellsConcentration:100nMIncubationTime:1hourResult:SubstantiallyreducedtheLIFactivationofSTAT3,reducedtheSTAT3activationbyOSMandCNTF,decreasedthephosphorylationofAKT,mTOR,S6,andERK1/2inbothBT-549andMDA-MB-231cellsandincreasedthephosphorylationofproapoptoticp38MAPKinBT549cells.體內(nèi)研究EC359(5mg/kg;subcutaneousinjection;3daysperweek;for25days;femaleathymicnudemice)treatmentsignificantlyreducesthetumorprogression.ThebodyweightsofmiceinEC359-treatedgroupsremainsunchangedconfirmingthelowtoxicityofEC359[1].AnimalModel:8-week-oldfemaleathymicnudemicewithMDA-MB-231cells[1]Dosage:5mg/kgAdministration:Subcutaneousinjection;3daysperweek;for25daysResult:Significantlyreducedthetumorprogression.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JClinInvest.2022Aug1;132(15):e157678.?AdvSci(Weinh).2021Feb25;8(9):2003535.?Cells.2022,11(21):3482.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ViswanadhapalliS,etal.EC359:AFirst-in-ClassSmall-MoleculeInhibitorforTargetingOncogenicLIFRSignalinginTriple-NegativeBreastCancer.MolCancerTher.2019Aug;18(8):1341-1354.McePdfHei