Millepachine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEMillepachineCat.No.:HY-N7591CASNo.:1393922-01-4分⼦式:C₂₂H₂₂O₄分⼦量:350.41作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY⽣物活性Millepachine来⾃中草药MillettiapachycarpaBenth的⽣物活性天然查尔酮，在体内外对多种⼈类癌细胞均显⽰出强⼤的抗肿瘤作⽤。体外研究Millepachine(1.25-20μM;48h)remarkablyinhibitstheproliferationofcisplatin-resistantA2780CPcells[1].Millepachine(2-8μM;24or48h)inducesG2/Marrestandapoptosiscisplatin-sensitiveA2780Sandcisplatin-resistantA2780CPcells[1].Millepachine(2-8μM;24h)decreasestopoisomeraseIIlevelsinA2780SandA2780CPcells[1].Millepachine(2-8μM;24h)inhibitsATP-bindingcassettetransporteractivityinA2780CPcells[1].CellProliferationAssay[1]CellLine:A2780CPcellsConcentration:0,1.25,2.5,5,10,20μMIncubationTime:48hoursResult:InhibitedthecellsproliferationwithanIC50of4μM.CellCycleAnalysis[1]CellLine:A2780SandA2780CPcells1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:2,4,8μMIncubationTime:24or48hoursResult:InducedsignificantG2/Marrestbothinbothcells.ThepercentageofcellsintheG2/Mfractionincreasedfrom15.99%invehiclecellsto24.93%,60.67%,and77.31%atdoseof2,4,and8μMinA2780Scells,respectively.ApoptosisAnalysis[1]CellLine:A2780SandA2780CPcellsConcentration:2,4,8μMIncubationTime:24or48hoursResult:Thepercentageofapoptoticcellsincreasedfrom1.49%invehiclecellsto10.98%,20.60%,and39.43%atdoseof2,4,and8μMinA2780Scells,respectively.Thepercentageofapoptoticcellsincreasedfrom0.87%to10.97%,25.28%,and37.59%inA2780CPcells,respectively.WesternBlotAnalysis[1]CellLine:A2780SandA2780CPcellsConcentration:0,2,4,8μMIncubationTime:24hoursResult:DecreasedthelevelsoftopoisomeraseII(TOPOII)inbothcells.体内研究Millepachine(20mg/kg;i.v.everytwodaysfor14day)inhibitstumorgrowthinmice[1].Millepachine(20mg/kg;i.v.everytwodaysfor14day)doesnotinduceacquireddrugresistanceinanexcisedA2780Sxenograftmodel[1].AnimalModel:FemaleBALB/cnudemice(6weeks)areinjectedA2780SorA2780CPcells[1]Dosage:20mg/kgAdministration:I.v.everytwodaysfor2-14daysResult:Reducedtumorvolumeandtumorweightwiththeinhibitoryrateof73.21%and65.58%inA2780S(afterseventimesinjection)andA2780CP(aftersixtimesinjection)xenograftmodel,respectively.Withlowtoxicityinvivo.REFERENCES2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].WuW,et,al.Millepachineshowednovelantitumoreffectsincisplatin-resistanthumanovariancancerthroughinhibitingdrugeffluxfunctionofATP-bindingcassettetransporters.PhytotherRes.2018Dec;32(12):2428-2435.McePdfHeightCaution:Producthasnotbeenfullyvalidatedforme