Decitabine-5-Aza-2-deoxycytidine-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDecitabineCat.No.:HY-A0004CASNo.:2353-33-5Synonyms:5-Aza-2'-deoxycytidine;5-AZA-CdR;NSC127716分?式:C?H??N?O?分?量:228.21作?靶點(diǎn):DNAMethyltransferase;Apoptosis;NucleosideAntimetabolite/Analog作?通路:Epigenetics;Apoptosis;CellCycle/DNADamage儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥50mg/mL(219.10mM)H2O:20mg/mL(87.64mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.3819mL21.9096mL43.8193mL5mM0.8764mL4.3819mL8.7639mL10mM0.4382mL2.1910mL4.3819mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(10.95mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(10.95mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(10.95mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:10mg/mL(43.82mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Decitabine(5-Aza-2'-deoxycytidine)?種具有?服活性的脫氧胞苷類似物抗代謝物(deoxycytidineanalogueantimetabolite)和DNA甲轉(zhuǎn)移酶(DNAmethyltransferase)抑制劑。Decitabine代替DNA摻?胞嘧啶可以將DNA甲轉(zhuǎn)移酶共價(jià)捕獲到DNA中，從?導(dǎo)致對(duì)該酶的不可逆抑制。Decitabine誘導(dǎo)細(xì)胞G2/M阻滯和細(xì)胞凋亡(apoptosis)，并具有有效的抗癌活性。IC50&TargetDNMT1DNMT3ADNMT3B體外研究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.體內(nèi)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?邊的抑制劑?師www.MedChemEDosage:1.0mg/kgAdministration:Intraperitonealinjection;oncedailyfor5consecutivedaysResult:CausedcontinuoustumorregressionevenafterDecitabinetreatmentwasstopped.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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