Camptothecin-Campathecin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECamptothecinCat.No.:HY-16560CASNo.:7689-03-4Synonyms:Campathecin;(S)-(+)-Camptothecin;CPT分⼦式:C₂₀H₁₆N₂O₄分⼦量:348.35作⽤靶点:Topoisomerase;ADCCytotoxin;MicroRNA;InfluenzaVirus;Apoptosis;Fungal;Antibiotic作⽤通路:CellCycle/DNADamage;Antibody-drugConjugate/ADCRelated;Epigenetics;Anti-infection;Apoptosis储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:6.25mg/mL(17.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8707mL14.3534mL28.7068mL5mM0.5741mL2.8707mL5.7414mL10mM0.2871mL1.4353mL2.8707mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性Camptothecin(CPT)，⼀种⽣物碱，⼀种DNAtopoisomeraseI(TopoI)抑制剂，其IC50值为679nM[1]。Camptothecin(CPT)对结直肠癌、乳腺癌、肺癌和巢癌具有强⼤的抗肿瘤活性，通过改变⼈类癌细胞中的miRNA表达模式来调节hypoxia-induciblefactor-1α(HIF-1α)活性[2][3]。1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50&TargetTopoisomeraseICamptothecins679nM(IC50)体外研究HighTOP1enzymaticactivityMCF7(Luminalsubtype)andHCC1419(HER2subtype)showhighsensitivitytowardCamptothecin(0.1ꢀμMto5ꢀμM;72ꢀhours)treatment,exhibitingtheIC50valuesof0.089ꢀμMand0.067ꢀμM,respectively[4].Camptothecin(0.5ꢀμM;6and24hours)reducesdesferrioxamine-activatedVEGFexpression.Camptothecin(0.5ꢀμM;8to24hours)stronglypreventsthedesferrioxamine-dependentHIF-1aaccumulation[2].CellViabilityAssay[4]CellLine:MCF7(Luminalsubtype)andHCC1419(HER2subtype)Concentration:0.1ꢀμMto5ꢀμMIncubationTime:72ꢀhoursResult:HighTOP1enzymaticactivityMCF7(Luminalsubtype)andHCC1419(HER2subtype)showhighsensitivitytowardCPT(0.1ꢀμMto5ꢀμM;72ꢀhours)treatment,exhibitingtheIC50valuesof0.089ꢀμMand0.067ꢀμM,respectively.RT-PCR[2]CellLine:HeLaandHEK293celllinesConcentration:0.5μmol/LIncubationTime:6and24hoursResult:Reducesdesferrioxamine-activatedVEGFexpressioninbothcelllinesafter6and24hoursoftreatment,whereasinnormoxicconditioncamptothecindoesnotaffecttheVEGFmRNAlevel.WesternBlotAnalysis[2]CellLine:HeLaandHEK293celllinesConcentration:0.5μmol/LIncubationTime:8to24hoursResult:Stronglypreventsthedesferrioxamine-dependentHIF-1aaccumulationafter8to24hours,whereasitdoesnotaffectHIF-1blevels.体内研究Camptothecin(2mg/kgeveryotherday)treatsmice,hasdevelopednumerouspulmonarymetastases.Treatmentwithbothkinaseinhibitorofnuclearfactor-kappaB-1(KINK-1)andCamptothecinledtoastatisticallysignificantreductioninthenumberofpulmonarymetastases[5].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:C57BL6mice(injectedwithB16F10melanomacells)[5]Dosage:2mg/kgAdministration:everyotherday,after19daysResult:Hasdevelopednumerouspulmonarymetastases.户使⽤本产品发表的科研⽂献•Immunity.2022Aug9;55(8):1370-1385.e8.•NatCommun.2022Aug16;13(1):4822.•NatCommun.2021Aug16;12(1):4961.•NatCommun.2019Aug21;10(1):3761.•NatCommun.2018Oct8;9(1):4139.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LuzzioMJ,etal.SynthesisandantitumoractivityofnovelwatersolublederivativesofcamptothecinasspecificinhibitorsoftopoisomeraseI.SynthesisandantitumoractivityofnovelwatersolublederivativesofcamptothecinasspecificinhibitorsoftopoisomeraseI.[2].BertozziD,etal.ThenaturalinhibitorofDNAtopoisomeraseI,camptothecin,modulatesHIF-1αactivitybychangingmiRexpressionpatternsinhumancancercells.MolCancerTher.2014;13(1):239-248.[3].SchönM,etal.KINK-1,anovelsmall-moleculeinhibitorofIKKbeta,andthesusceptibilityofmelanomacellstoantitumoraltreatment.JNatlCancerInst.2008;100(12):862-875..[4].HuangQ,etal.EvolutioninmedicinalchemistryofE-ring-modifiedCamptothecinanalogsasanticanceragents.EurJMedChem.2013;63:746-757.[5].TesauroC,etal.TopoisomeraseIactivityandsensitivitytocamptothecininbreastcancer-derivedcells:acomparativestudy.BMCCancer.2019;19(1):1158.Published2019No