Doxorubicin-hydrochloride-Hydroxydaunorubicin-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDoxorubicinhydrochlorideCat.No.:HY-15142CASNo.:25316-40-9Synonyms:Hydroxydaunorubicinhydrochloride;HydroxydaunorubicinHydrochloride分⼦式:C₂₇H₃₀ClNO₁₁分⼦量:579.98作⽤靶点:Topoisomerase;ADCCytotoxin;AMPK;Autophagy;Apoptosis;HIV;HBV;Mitophagy;Antibiotic;Bacterial作⽤通路:CellCycle/DNADamage;Antibody-drugConjugate/ADCRelated;Epigenetics;PI3K/Akt/mTOR;Autophagy;Apoptosis;Anti-infection储存⽅式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:35.71mg/mL(61.57mM;ultrasonicandwarmingandheatto60°C)H2O:20mg/mL(34.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7242mL8.6210mL17.2420mL5mM0.3448mL1.7242mL3.4484mL10mM0.1724mL0.8621mL1.7242mL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(sealedstorage,awayfrommoistureandlight)。-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。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.59mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.59mM);Clearsolution3.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.75mg/mL(4.74mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Doxorubicin(Hydroxydaunorubicin)hydrochloride⼀种具有细胞毒性的蒽环类抗⽣素，⼀种抗癌化疗试剂。Doxorubicinhydrochloride⼀种有效的⼈类DNAtopoisomeraseI和topoisomeraseII抑制剂，IC50分别为0.8μM和2.67μM。Doxorubicinhydrochloride可降低AMPK及其下游靶蛋⽩⼄酰辅酶A羧化酶的磷酸化。还可诱导凋亡(apoptosis)和⾃噬[1][2][3]。IC50&TargetTopoisomeraseITopoisomeraseIIDaunorubicins/DoxorubicinsHIV-10.8μM(IC50)2.67μM(IC50)体外研究Doxorubicinhydrochloride(1-8µM;24and48hours)decreasestheviabilityofMCF-10F,MCF-7andMDA-MB-231cellsinatime-anddose-dependentmanner[4].Doxorubicinhydrochloride(1μM;3and24hours)resultsinHct-116humancoloncarcinomacellsreductioninG0/G1phaseandaccumulationinG2phase[5].Doxorubicinhydrochloride(1μMforMCF-10FandMDA-MB-231cells,4μMforMCF-7cells;48hours)inducesapoptosisbyupregulatingBax,caspase-8andcaspase-3anddownregulationofBcl-2proteinexpression[4].CellViabilityAssay[4]CellLine:BreastcancercelllinesMCF-10F,MCF-7andMDA-MB-231Concentration:0,1,2,4and8μMIncubationTime:24and48hoursResult:IC50was1μMforbothMCF-10FandMDA-MB-231celllines.IC50was4μMforMCF-7cellline.CellCycleAnalysis[5]CellLine:Hct-116humancoloncarcinomacellsConcentration:1μMIncubationTime:3hoursand24hoursResult:Both,bolus(3h)andcontinuous(24h)incubationledtoasignificantreductionofcellsin2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEG0/G1andaccumulationinG2phase.WesternBlotAnalysis[4]CellLine:BreastcancercelllinesMCF-10F,MCF-7andMDA-MB-231Concentration:1μMforMCF-10FandMDA-MB-231cells,4μMforMCF-7cellsIncubationTime:48hoursResult:BaxproteinexpressionwasupregulatedinMCF-10FandMDA-MB-231celllinesbutMCF-7cellsdidnotshowanysignificantincrease.Caspase-8geneexpressionwasupregulatedinMCF-10F,butitwasdownregulatedinMCF-7andMDA-MB-231cells.体内研究TreatmentwithDoxorubicin(2mg/kg)orZoledronicacid(100μg/kg)alonedoesnotstatisticallysignificantlydecreasefinaltumorvolumecomparedwithsaline.MicetreatedwithDoxorubicinplusZoledronicacidhavestatisticallysignificantlysmallerfinaltumorvolumesthanthosetreatedwithDoxorubicinalone[6].AnimalModel:FemaleMF1nu/numicebearingMDA-G8breasttumorxenograft(6-week-old)[6]Dosage:Doxorubicin(2mg/kg);Zoledronicacid(100μg/kg)Administration:Intravenousinjection;onceaweek;6weeksResult:Moderateinhibitionofsubcutaneoustumorgrowthinmicethatweretreatedwith2mg/kgDoxorubicinaloneorwith100μg/kgZoledronicacidalonecomparedtothesalinecontrol.MicetreatedwithZoledronicacidandDoxorubicintogetherhadstatisticallysignificantsmallermeantumorvolumesonday42thanthosetreatedwithDoxorubicinalone.户使⽤本产品发表的科研⽂献•NatMed.2016May;22(5):547-56.•CellRes.2018Dec;28(12):1171-1185.•MilMedRes.2021Dec9;8(1):63.•CellMetab.2022Feb7;34(3):424-440.e7.•NatCellBiol.2020Sep;22(9):1056-1063.Seemorecustomervalidationsonwww.MedChemEREFERENCES3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].JohnL.Nitiss,etal.TargetingDNAtopoisomeraseIIincancerchemotherapy.NatRevCancer.2009May;9(5):338-50.[2].Hee-KyungRhee,etal.Synthesis,cytotoxicity,andDNAtopoisomeraseIIinhibitoryactivityofbenzofuroquinolinediones.BioorgMedChem.2007Feb15;15(4):1651-8.[3].PDFoglesong,etal.DoxorubicininhibitshumanDNAtopoisomeraseI.CancerChemotherPharmacol.1992;30(2):123-5.[4].NesstorPilco-Ferreto,etal.Influenceofdoxorubicinonapoptosisandoxidativestressinbreastcancercelllines.IntJOncol.2016Aug;49(2):753-62.[5].RegineLüpertz,etal.Dose-andtime-dependenteffectsofdoxorubicinoncytotoxicity,cellcycleandapoptoticcelldeathinhumancoloncancercells.Toxicology.2010May27;271(3):115-21.[6].PenelopeDOttewell,etal.Antitumoreffectsofdoxorubicinfollowedbyzoledronicacidinam