BIM-46068-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBIM-46068Cat.No.:HY-117893CASNo.:201487-53-8分⼦式:C₂₁H₄₂N₄O₃S₃分⼦量:494.78作⽤靶点:FarnesylTransferase作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性BIM-46068⼀种强效的、选择性的⼈脑法尼转移酶(FTase)抑制剂(IC50=91.4nM)。BIM-46068可特异性抑制MiaPaCa-2癌细胞中的Ras加⼯。BIM-46068可⽤于胰腺癌的研究[1]。体外研究BIM-46068(0.1-10µM,48h)specificallyinhibitstheprocessingofRasinMiaPaCa-2cancercells[1].BIM-46068(96h)inhibitsthegrowthofcellsbearingthewild-typerasaswellascellswiththedifferentmutatedras(K-ras,N-ras,orH-ras)andeffectivelyinhibitsthemultidrug-resistantcelllineT24R[1].WesternBlotAnalysis[1]CellLine:MiaPaCa-2cellsConcentration:0.1µM,1µM,10µMIncubationTime:48hResult:CausedachangeintheelectrophoreticmigrationrateofH-RasproteininMiaPaCa-2cells,fromrapidmigration(farnesylatedform)toslowmigration(unfarnesylatedform).体内研究BIM-46068(1-30mg/kg,i.p.,oncedailyfor10days)significantlyreducestumorgrowthinadose-dependentmanner,andnosignsoftoxicity,suchasweightlossordeath,areobservedatthehighestdose(30mg/kg)[1].AnimalModel:Nudemicewereimplanteds.c.withMiaPaCa-2cells(5×106),ahumanpancreatictumorcelllineexpressingmutatedK-ras[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:1mg/kg,10mg/kg,30mg/kgAdministration:I.p.,oncedailyfor10daysResult:Significantlyreducedtumorgrowthinadose-dependentmanner.Onday34post-implantation,themeantumorvolumeinthe30mg/kggroupwasreducedby50%comparedtothecontrolgroup.REFERENCES[1].PrevostGP,etal.Inhibitionofhumantumorcellgrowthinvitroandinvivobyaspecificinhibitorofhumanfarnesyltransferase:BIM-46068.IntJCancer.1999Oct8;83(2):283-7.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-