Sparfosic-acid-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESparfosicacidCat.No.:HY-112732CASNo.:51321-79-0分⼦式:C₆H₁₀NO₈P分⼦量:255.12作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验H2O:125mg/mL(489.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.9197mL19.5986mL39.1972mL5mM0.7839mL3.9197mL7.8394mL10mM0.3920mL1.9599mL3.9197mLBIOLOGICALACTIVITY⽣物活性SparfosicacidDNA抗代谢剂和天门冬氨酸氨甲酰转移酶(aspartatetranscarbamoyltransferase)的有效抑制剂。Sparfosicacid具有抗肿瘤活性。天冬氨酸氨甲酰转移酶催化第⼆步denovo嘧啶⽣物合成。体外研究Sparfosicacid(PALA)causesapoptosisintheresistantBr1cells[1].Sparfosicacid(300µM)showsprogressiveaccumulationofcellsinSphaseandactivationofanapoptoticpathwayleadingtocelldeath[1].CellViabilityAssay[1]CellLine:Br-landL-2celllinesestablishedfrommetastasisinnudemouseinjectedwiththehumantumorcelllineMDA-MB-4351/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:300µMIncubationTime:12,24and48hoursResult:CellswerepredominantlyinSphaseinboththecelllines,althoughslightlyhigherproportionofcellsinSphasewerenotedinL-2thanBrl-3prlcells.WesternBlotAnalysis[1]CellLine:Br-landL-2celllinesConcentration:300µMIncubationTime:4,10and24hoursResult:TherewasmoderatedifferenceinthelevelofphosphorylatedRbproteinsseeninthetwocelltypes.MarkedincreaseintheamountofcyclinAproteinwasdetectedintheL-2cellsundergoingapoptosiswiththehighestleveldetectedat10hpost-drugtreatment.Incontrast,therewasnoincreaseinthelevelofcyclinAseenintheBrl-3prlcells.CyclinEproteinwasfoundelevatedintheL-2cellsandBrl-3prlcellscomparedtotheirrespectivecontrols.REFERENCES[1].WangJ,etal.ElevatedcyclinAassociatedkinaseactivitypromotessensitivityofmetastatichumancancercellstoDNAantimetabolitedrug.IntJOncol.2015Aug;47(2):782-90.[2].AngelaD.Morris,etal.ANew,Efficient,TwoStepProcedureforthePreparationoftheAntineoplasticAgentSparfosicAcid.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon