SR18662-DataSheet-生命科學(xué)試劑-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemESR18662Cat.No.:HY-136530分?式:C??H??Cl?N?O?S分?量:420.31作?靶點(diǎn):KLF作?通路:MAPK/ERKPathway儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(297.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3792mL11.8960mL23.7920mL5mM0.4758mL2.3792mL4.7584mL10mM0.2379mL1.1896mL2.3792mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請(qǐng)先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.95mM);Clearsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.95mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性SR18662?種有效的Kruppel-likefactor5(KLF5)的抑制劑，IC50為4.4nM，ML264(HY-19994)的類似物。SR18662可?于結(jié)直腸癌的相關(guān)研究。IC50&TargetIC50:4.4nM(KLF5)[1]體外研究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.體內(nèi)研究SR18662(intraperitonealinjection;5-10mg/kg;dailyortwicedaily;5daysinjection,daysbreak,and5days)significantlyreducesthegrowthoftumorsinamousexenograftmodel[1].AnimalModel:NudemicewithDLD-1cells[1]2/3MasterofSmallMolecules—您?邊的抑制劑?師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