Indimitecan-LMP776-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIndimitecanCat.No.:HY-18350CASNo.:915360-05-3Synonyms:LMP776分?式:C??H??N?O?分?量:459.45作?靶點(diǎn):Topoisomerase作?通路:CellCycle/DNADamage儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:8.33mg/mL(18.13mM;ultrasonicandwarmingandadjustpHto3withHClandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1765mL10.8826mL21.7652mL5mM0.4353mL2.1765mL4.3530mL10mM0.2177mL1.0883mL2.1765mLBIOLOGICALACTIVITY?物活性Indimitecan(LMP776)?種拓?fù)洚悩?gòu)酶I(Top1)抑制劑，具有抗癌活性。IC50&TargetTop1體外研究Indimitecan(LMP776)(0-100μM)showsantiproliferativepotenciesagainstvarioushumancancercelllines,withmean-graphmidpoint(MGM)of0.079±0.023μM[1].IndimitecanshowspotentDNAcleavageduetoTop1inhibition[1].Indimitecancanbesubstratesformetabolicketonereductases[1].CellProliferationAssay[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師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