SR18662-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESR18662Cat.No.:HY-136530分⼦式:C₁₆H₁₉Cl₂N₃O₄S分⼦量:420.31作⽤靶点:KLF作⽤通路:MAPK/ERKPathway储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(297.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3792mL11.8960mL23.7920mL5mM0.4758mL2.3792mL4.7584mL10mM0.2379mL1.1896mL2.3792mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.95mM);Clearsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.95mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性SR18662⼀种有效的Kruppel-likefactor5(KLF5)的抑制剂，IC50为4.4nM，ML264(HY-19994)的类似物。SR18662可⽤于结直肠癌的相关研究。IC50&TargetIC50:4.4nM(KLF5)[1]体外研究SR18662(0-10μM;24-72hours)significantlyreducesgrowthandproliferationofCRCcellsascomparedtotreatmentwithvehiclecontrol,ML264(HY-19994).ItshowsimprovedefficacyinreducingviabilityofmultipleCRCcelllines[1].SR18662(10μM;24-72hours)showsasignificantincreaseinthenumberofapoptoticcellsatbothearlyandlatestatesinDLD-1andHCT116cells[1].SR18662(1μM;72hours)reducestheexpressionofcyclins(cyclinsE,A2,andB1)andcomponentsofMAPK(p-Erk)andWNTsignalingpathways(p-GSK3β)incells[1].CellViabilityAssay[1]CellLine:CRCcellsConcentration:0-10μMIncubationTime:24hours,48hours,72hoursResult:Inducedanti-tumoractivityincolorectalcancercelllines.ApoptosisAnalysis[1]CellLine:DLD-1andHCT116cellsConcentration:10μMIncubationTime:24hours,48hours,72hoursResult:Increasedapoptosisofcolorectalcancercelllines.WesternBlotAnalysis[1]CellLine:DLD-1andHCT116cellsConcentration:1μMIncubationTime:72hoursResult:ReducedlevelsofcyclinsE,A2,andB1inhibitsactivityofMAPK,WNT/β-cateninsignalingpathwaysanddecreasesthelevelsofcyclins.体内研究SR18662(intraperitonealinjection;5-10mg/kg;dailyortwicedaily;5daysinjection,daysbreak,and5days)significantlyreducesthegrowthoftumorsinamousexenograftmodel[1].AnimalModel:NudemicewithDLD-1cells[1]2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:5mg/kg;10mg/kg;25mg/kgAdministration:Intraperitonealinjection;5mg/kgdaily,5mg/kgtwiceaday,10mg/kgdaily,10mg/kgtwiceperday,25mg/kgdaily,and25mg/kgtwiceperday;5daysofinjections,2daysbreak,and5daysofinjectionsResult:Causedasignificantdose-dependentinhibitionofxenograftgrowthinmice.REFERENCES[1].JulieKim,etal.TheNovelSmall-MoleculeSR18662EfficientlyInhibitstheGrowthofColorectalCancerInVitroandInVivo.MolCancerTher.2019Nov;18(11):1973-1984.McePdfHeightCaution:Producthasnotbeenfullyvalidated