Decitabine-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEDecitabineCat.No.:HY-A0004CASNo.:2353-33-5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儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥50mg/mL(219.10mM)掃描?維碼，H2O:20mg/mL(87.64mM;Needultrasonic)運(yùn)?溶解?案計(jì)算器*"≥"meanssoluble,butsaturationunknown.獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.3819mL21.9096mL43.8193mL5mM0.8764mL4.3819mL8.7639mL10mM0.4382mL2.1910mL4.3819mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請根據(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?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(10.95mM);Clearsolution此?案可獲得≥2.5mg/mL(10.95mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)1/4www.MedChemEwww.MedChemESolubility:≥2.5mg/mL(10.95mM);Clearsolution此?案可獲得≥2.5mg/mL(10.95mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.5mg/mL(10.95mM);Clearsolution此?案可獲得≥2.5mg/mL(10.95mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。4.以1mL?作液為例，取100μL25.0mg/mL的澄請依序添加每種溶劑：PBSDMSO儲備液加到900μL??油中，混合均勻。Solubility: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].2/4www.MedChemEwww.MedChemEAnimalModel:C57BL/6mice(bearingEL4cells)[6]Dosage: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.?JAllergyClinImmunol.2019Jun;143(6):2038-2051.e12.?ProgNeurobiol.2021Feb23;102028.?Theranostics.2021Mar20;11(11):5605-5619.?Theranostics.2021;11(2):841-860.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.2009Jul;109(7):2880-93.McePdfHeight3/4www.MedChemEwww.MedChemE關(guān)注MCE中國公眾號，

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