Indimitecan-LMP776-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIndimitecanCat.No.:HY-18350CASNo.:915360-05-3Synonyms:LMP776分⼦式:C₂₅H₂₁N₃O₆分⼦量:459.45作⽤靶点:Topoisomerase作⽤通路:CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:8.33mg/mL(18.13mM;ultrasonicandwarmingandadjustpHto3withHClandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1765mL10.8826mL21.7652mL5mM0.4353mL2.1765mL4.3530mL10mM0.2177mL1.0883mL2.1765mLBIOLOGICALACTIVITY⽣物活性Indimitecan(LMP776)⼀种拓扑异构酶I(Top1)抑制剂，具有抗癌活性。IC50&TargetTop1体外研究Indimitecan(LMP776)(0-100μM)showsantiproliferativepotenciesagainstvarioushumancancercelllines,withmean-graphmidpoint(MGM)of0.079±0.023μM[1].IndimitecanshowspotentDNAcleavageduetoTop1inhibition[1].Indimitecancanbesubstratesformetabolicketonereductases[1].CellProliferationAssay[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:HOP-62,HCT-116,SF-539,UACC-62,OVCAR-3,SN12C,DU-145,MCF-7Concentration:0-100μMIncubationTime:Result:ShowedgrowthinhibitionwithGI50sof<0.01,<0.01,0.04,<0.01,0.08,<0.01,<0.01and0.01μMagainstHOP-62,HCT-116,SF-539,UACC-62,OVCAR-3,SN12C,DU-145andMCF-7cells,respectively.Andthemean-graphmidpoint(MGM)forgrowthinhibitionofallhumancancercelllinessuccessfullytested(theNationalCancerInstitute’sdevelopmentaltherapeuticsassay(the“NCI60”))was0.079±0.023μM.REFERENCES[1].CinelliMA,etal.Identification,synthesis,andbiologicalevaluationofmetabolitesoftheexperimentalcancertreatmentdrugsindotecan(LMP400)andindimitecan(LMP776)andinvestigationofisomericallyhydroxylatedindenoisoquinolineanaloguesastopoisomeraseIpoisons.JMedChem.2012Dec27;55(24):10844-62.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-82