CAY10404-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemECAY10404Cat.No.:HY-121537CASNo.:340267-36-9分⼦式:C₁₇H₁₂F₃NO₃S分⼦量:367.34作⽤靶点:COX;Akt;Apoptosis作⽤通路:Immunology/Inflammation;PI3K/Akt/mTOR;Apoptosis储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)BIOLOGICALACTIVITY⽣物活性CAY10404⼀种有效且⾼度选择性的环氧合酶2(COX-2)抑制剂，IC50为1nM。CAY10404对COX-1没有抑制作⽤(IC50>500µM)。CAY10404有效的PKB/Akt和MAPK信号通路抑制剂，可诱导NSCLC细胞凋亡(apoptosis)。CAY10404⼀种⼆芳异恶唑，具有良好的⽌痛，抗炎和抗癌活性。IC50&TargetCOX-2COX-1Akt1nM(IC50)>500μM(IC50)体外研究CAY10404isapotentandselectiveCOX-2inhibitorwithaselectivityindex(SI;COX-1IC50/COX-2IC50)of>500000[1].CAY10404(10-100µM;for3days)inhibitsthegrowthofNSCLCcelllinesinaconcentration-dependentmannerandhasanaverage50%inhibitoryconcentration(IC50)of60-100µM[3].CAY10404(20-100µM;for3days)inducesapoptosisinNSCLCcells[3].CAY10404(80µM;for3days)inducesaconcentration-dependentdecreaseintheleveloftheanti-apoptoticproteins(Bcl-2andBcl-XL)andpAktandpGSK-3β[3].CAY10404(20,50,80,100µM;for14days)compromisestheabilityofH460cellstoformcoloniesinanchorage-independentgrowthinaconcentration-dependentmanner[3].CellViabilityAssay[3]CellLine:Non-smallcelllungcancer(NSCLC)cells(H-1703,H-358,H-460)Concentration:10-100µM1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:For3daysResult:InhibitedthegrowthofNSCLCcelllinesinaconcentration-dependentmanner.ApoptosisAnalysis[3]CellLine:H460cellsConcentration:20,50,100µMIncubationTime:For3daysResult:InducedapoptosisinNSCLCcells.WesternBlotAnalysis[3]CellLine:NSCLCcells(H-358,H-460)Concentration:80µMIncubationTime:For3daysResult:Inducedaconcentration-dependentdecreaseintheleveloftheanti-apoptoticproteins(Bcl-2andBcl-XL)andpAktandpGSK-3β,withoutchangingthelevelofthepro-apoptoticprotein(Bax)andtotalAktandGSK-3βproteinlevels.体内研究CAY10404(50mg/kg/day;ip;for4days)decreaseslunginflammationinHTVmiceandattenuatesventilator-inducedlunginjury[2].AnimalModel:AdultmaleC57Bl/6Jmiceweighing24-30g[2]Dosage:50mg/kgAdministration:IP;daily;for4daysResult:Attenuatedcyclooxygenaseactivity,significantlydecreasingBALPGE2and6-ketoPGF1α.DecreasedlunginflammationinHTVmice(hightidalvolume;20ml/kg;for4hours)andattenuatesventilator-inducedlunginjury.REFERENCES[1].AGHabeeb,etal.Designandsynthesisof4,5-diphenyl-4-isoxazolines:novelinhibitorsofcyclooxygenase-2withanalgesicandantiinflammatoryactivity.JMedChem.2001Aug30;44(18):2921-7.[2].JoshuaARobertson,etal.Theroleofcyclooxygenase-2inmechanicalventilation-inducedlunginjury.AmJRespirCellMolBiol.2012Sep;47(3):387-94.2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE[3].YongseonCho,etal.EffectsofCAY10404onthePKB/AktandMAPKpathwayandapoptosisinnon-smallcelllungcancercells.Respirology.2009Aug;14(6):850-8.McePdfHeightCaution:Producthasnotbeenfullyval