SP-141-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESP-141Cat.No.:HY-110182CASNo.:1253491-42-7分⼦式:C₂₂H₁₆N₂O分⼦量:324.38作⽤靶点:MDM-2/p53作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(385.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0828mL15.4140mL30.8280mL5mM0.6166mL3.0828mL6.1656mL10mM0.3083mL1.5414mL3.0828mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.41mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.41mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性SP-141⼀种特异性的MDM2抑制剂。SP-141促进MDM2⾃泛素化和降解。SP-141可⽤于胰腺癌和乳腺癌的研究[1]。IC50&TargetMDM2[1]体外研究SP-141(0.01-10μM;72hours)inhibitshumanpancreaticcancercellgrowthwithIC50valuesoflessthan0.5μM(0.38-0.50μM)inap53-independentmanner.TheIMR90cellsaremuchlesssensitivetoSP141thanthepancreaticcancercells,suggestingthatSP141hasaselectivecytotoxicityforcancercells[1].SP141inducesMDM2auto-ubiquitinationandproteasomaldegradationinbothHPACandPanc-1cells[1].CellViabilityAssay[1]CellLine:HPAC,Panc-1,AsPC-1,andMia-Paca-2pancreaticcancercelllines.Humanprimaryfibroblasts(IMR90)Concentration:0.01,0.1,1,and10μMIncubationTime:72hoursResult:IC50sof0.38,0.50,0.36,0.41,and13.22μMforHPAC,Panc-1,AsPC-1,Mia-Paca-2,andIMR90,respectively.WesternBlotAnalysis[1]CellLine:HPACandPanc-1cellsConcentration:0.5μMIncubationTime:120minutesResult:ReducedtheMDM2proteinlevels.IncreasedthedegradationrateoftheMDM2proteininthepresenceofCycloheximide(15μg/mL).体内研究SP-141(40mg/kg;administeredbyi.p.injection;5d/wkforaboutthreeweeks)suppressespancreatictumorgrowthinbothxenograftandorthotopicmousemodels[1].AnimalModel:NudemicebearingPanc-1xenografttumors[1]Dosage:40mg/kgAdministration:Administeredbyi.p.injection;5d/wkforaboutthreeweeksResult:Significantlysuppressedthegrowthofpancreaticxenografttumors.OnDay18,thetumorvolumeinthetreatedgroupwasreducedby75%comparedwiththatinthecontrolgroup.Therewerenosignificantdifferencesinthebodyweightcomparedwiththecontrolgroup.2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].WeiWang,etal.IdentificationofaNewClassofMDM2InhibitorThatInhibitsGrowthofOrthotopicPancreaticTumorsinMice.Gastroenterology.2014Oct;147(4):893-902.e2.[2].WeiWang,etal.ThePyrido[b]indoleMDM2InhibitorSP-141ExertsPotentTherapeuticEffectsinBreastCancerModels.NatCommun.2014Oct1;5:5086.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf