Belotecan-CKD-602-free-base-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBelotecanCat.No.:HY-13566CASNo.:256411-32-2Synonyms:CKD-602freebase分⼦式:C₂₅H₂₇N₃O₄分⼦量:433.5作⽤靶点:Topoisomerase;Apoptosis作⽤通路:CellCycle/DNADamage;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Belotecan(CKD-602freebase)DNAtopoisomeraseI抑制剂。Belotecan诱导细胞凋亡以及周期阻滞。Belotecan⼀种具有抗肿瘤效应的喜树碱衍⽣物，可⽤于癌症的研究。IC50&TargetIC50:30ng/mL(Caskicells),150ng/mL(HeLacells),150ng/mL(SiHacells)[1]体外研究Belotecan(0-600ng/mL;0-72h)time-anddose-dependentlyinhibitsviabilityofCaskicells,HeLacellsandSiHacellsat48hwithIC50valuesof30,150and150ng/mL,respectively[1].Belotecan(0-150ng/mL;48h)inducescellapoptosisandcell-cyclearrest,andaffectsPARP,cleavedPARP,BAX,p53,Ser15,cellcyclerelatedproteinexpressionandcancerinvasionincervicalcancer[1].ApoptosisAnalysis[1]CellLine:Caski,HeLaandSiHacelllinesConcentration:0-150ng/mLIncubationTime:48hResult:Showedstrongpro-apoptoticactivitiestoCaski,HeLaandSiHacells.WesternBlotAnalysis[1]CellLine:Caski,HeLaandSiHacelllines1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:0-150ng/mLIncubationTime:48hResult:IncreasedtheexpressionofPARP,cleavedPARP,BAX,p53,Ser15,cyclinB1,phosphorylatedcyclinB1andphospho-cdc2(Tyr15)protein,anddecreasedMMP2andVEGFproteinexpression.CellCycleAnalysis[1]CellLine:Caski,HeLaandSiHacelllinesConcentration:0-150ng/mLIncubationTime:48hResult:Inducedcell-cyclearrestintheG2/Mphaseincervicalcancer.CellInvasionAssay[1]CellLine:Caski,HeLaandSiHacelllinesConcentration:0-150ng/mLIncubationTime:48hResult:Inhibitedcancerinvasionincervicalcancer.体内研究Belotecan(25mg/kg;i.v.for16daysat4-dayintervals)inhibitstumorgrowthinCaSki-xenograftsnudemice[1].AnimalModel:BALB/c-nudemicewithCaSkicellsinjection[1]Dosage:25mg/kgAdministration:Intravenousinjection;25mg/kg;16daysat4-dayintervalsResult:Significantlyinhibitedthetumorgrowthandshowednosignificantdifferenceinbodyweightofxenograftmiceandthecontrols.户使⽤本产品发表的科研⽂献•JMolMed(Berl).2019Aug;97(8):1183-1193.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].LeeS,etal.CKD-602,atopoisomeraseIinhibitor,inducesapoptosisandcell-cyclearrestandinhibitsinvasionincervicalcancer.MolMed.2019May28;25(1):23.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio