Decitabine-5-Aza-2-deoxycytidine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDecitabineCat.No.:HY-A0004CASNo.:2353-33-5Synonyms:5-Aza-2'-deoxycytidine;5-AZA-CdR;NSC127716分⼦式:C₈H₁₂N₄O₄分⼦量:228.21作⽤靶点:DNAMethyltransferase;Apoptosis;NucleosideAntimetabolite/Analog作⽤通路:Epigenetics;Apoptosis;CellCycle/DNADamage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:≥50mg/mL(219.10mM)H2O:20mg/mL(87.64mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM4.3819mL21.9096mL43.8193mL5mM0.8764mL4.3819mL8.7639mL10mM0.4382mL2.1910mL4.3819mL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。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、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(10.95mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(10.95mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(10.95mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:10mg/mL(43.82mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Decitabine(5-Aza-2'-deoxycytidine)⼀种具有⼝服活性的脱氧胞苷类似物抗代谢物(deoxycytidineanalogueantimetabolite)和DNA甲转移酶(DNAmethyltransferase)抑制剂。Decitabine代替DNA掺⼊胞嘧啶可以将DNA甲转移酶共价捕获到DNA中，从⽽导致对该酶的不可逆抑制。Decitabine诱导细胞G2/M阻滞和细胞凋亡(apoptosis)，并具有有效的抗癌活性。IC50&TargetDNMT1DNMT3ADNMT3B体外研究DecitabinetreatmentsignificantlyinhibitscellgrowthofSNU719,NCC24andKATOIII96hoursafterexposuretodecitabine.DecitabineinducesG2/MarrestandapoptosisinEBVaGC,inhibitsinvasionability,andup-regulatesE-cadherinexpressionforEBVaGC[1].Onlyhighconcentrations(10µM)Decitabine(0.1-1μM;24-72hours)resultsinaG2phasearrest,whichisaccompaniedbyareductionofcellsinG1phase[3].Decitabineup-regulatesDCTPP1anddUTPaseexpressioninHeLacells[4].CellCycleAnalysis[1]CellLine:HCT116cellsConcentration:0.1,1,10µMIncubationTime:24,48,72hoursResult:Onlyhighdrugconcentrations(10µM)resultedinaG2phasearrest,whichwasaccompaniedbyareductionofcellsinG1phase.体内研究Decitabine(1.0mg/kg,p.o.)incombinationwithtetrahydrouridine(THU)causesseveretoxicityoccursinfemaleCD-1mice,andresultsinanincreasedsensitivitytodecitabinetoxicitycorrelatingwithdecitabineplasmalevels[5].Decitabine(1.0mg/kg;i.p.;oncedailyfor5consecutivedays)leadstoregressionofEL4tumorsestablishedinC57BL/6Mice[7].AnimalModel:C57BL/6mice(bearingEL4cells)[6]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:1.0mg/kgAdministration:Intraperitonealinjection;oncedailyfor5consecutivedaysResult:CausedcontinuoustumorregressionevenafterDecitabinetreatmentwasstopped.户使⽤本产品发表的科研⽂献•AnnRheumDis.2019Oct;78(10):1420-1429.•NeuroOncol.2022Jun21;noac157.•Theranostics.2021Mar20;11(11):5605-5619.•Theranostics.2020Sep15;10(25):11444-11461.•JAllergyClinImmunol.2019Jun;143(6):2038-2051.e12.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].NakamuraM,etal.Decitabineinhibitstumorcellproliferationandup-regulatesE-cadherinexpressioninEpstein-Barrvirus-associatedgastriccancer.JMedVirol.2016Jul19.[2].HagemannS,etal.Azacytidineanddecitabineinducegene-specificandnon-randomDNAdemethylationinhumancancercelllines.PLoSOne.2011Mar7;6(3):e17388.[3].RequenaCE,etal.ThenucleotidohydrolasesDCTPP1anddUTPaseareinvolvedinthecellularresponsetodecitabine.BiochemJ.2016Jun20.[4].TerseP,etal.SubchronicoraltoxicitystudyofdecitabineincombinationwithtetrahydrouridineinCD-1mice.IntJToxicol.2014Mar-Apr;33(2):75-85.[5].YuJ,etal.DNAmethyltransferaseexpressionintriple-negativebreastcancerpredictssensitivitytodecitabine.JClinInvest.2018Jun1;128(6):2376-2388.[6].WangLX,etal.LowdosedecitabinetreatmentinducesCD80expressionincancercellsandstimulatestumorspecificcytotoxicTlymphocyteresponses.PLoSOne.2013May9;8(5):e62924.[7].ParkerWB.Enzymologyofpurineandpyrimidineantimetabolitesusedinthetreatmentofcancer.ChemRev.200