Cladribine-2-Chloro-2-deoxyadenosine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECladribineCat.No.:HY-13599CASNo.:4291-63-8Synonyms:2-Chloro-2′-deoxyadenosine;CldAdo;2CdA分⼦式:C₁₀H₁₂ClN₅O₃分⼦量:285.69作⽤靶点:AdenosineDeaminase;Apoptosis作⽤通路:MetabolicEnzyme/Protease;Apoptosis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:≥30mg/mL(105.01mM)H2O:10mg/mL(35.00mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5003mL17.5015mL35.0030mL5mM0.7001mL3.5003mL7.0006mL10mM0.3500mL1.7501mL3.5003mL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)1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：PBSSolubility:25mg/mL(87.51mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Cladribine(2-Chloro-2′-deoxyadenosine)⼀种嘌呤核苷类似物，具有⼝服活性的腺苷脱氨酶(adenosinedeaminase)抑制剂。Cladribine能作为DNA合成(DNAsynthesis)的抑制剂，可阻断受损DNA的修复。Cladribine可以抑制DNA甲化。Cladribine具有抗淋巴瘤活性，可⽤于⼀些⾎液恶性肿瘤和多发性硬化的研究[1][2]。IC50&TargetAdenosinedeaminase[2]体外研究Cladribine(0.25-4μM;24-48hours)inhibitshumanDLBCLcellsproliferation[1].Cladribine(1-4μM;24hours)inducesG1phasearrestviadecreasingtheexpressionsofCyclinD1andCyclinE,andincreasingtheexpressionsofp21andp27inDLBCLcells[1].Cladribine(1-4μM;24hours)inducesapoptosisandactivatesextrinsicandintrinsicsignalingpathwaysinhumanDLBCLcells[1].Cladribine(1-4μM;24hours)activatesendoplasmicreticulumstress[1].Cladribineinhibitscellproliferationofmultiplemyeloma(MM)cellsinadose-dependentmanner;withIC50sofapproximately2.43μM,0.75μMand0.18μMforU266,RPMI8226andMM1.Scells,respectively[2].CellProliferationAssay[1]CellLine:ThehumanDLBCLcelllines(U2932,OCI-LY10,SUDHL2,WSU-DLCL2,DB)Concentration:0μM,0.25μM,0.5μM,1μM,2μM,4μMIncubationTime:24hours,48hoursResult:ExhibitednotablesuppressionofcellproliferationinfiveDLBCLcells.WesternBlotAnalysis[1]CellLine:U2932cells,WSU-DLCL2cellsConcentration:0μM,1μM,2μM,4μMIncubationTime:24hoursResult:DecreasedtheexpressionsofCyclinD1andCyclinE,andincreasedtheexpressionsofp21andp27.ApoptosisAnalysis[1]CellLine:U2932cells,WSU-DLCL2cellsConcentration:0μM,1μM,2μM,4μM2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:24hoursResult:Inducedapoptosisandactivatesexogenousandendogenousapoptoticsignalingpathways.CellCycleAnalysis[1]CellLine:U2932cells,WSU-DLCL2cellsConcentration:0μM,1μM,2μM,4μMIncubationTime:24hoursResult:CausedG1phasearrest.RT-PCR[1]CellLine:U2932cells,WSU-DLCL2cellsConcentration:0μM,1μM,2μM,4μMIncubationTime:24hoursResult:ActivatedERstress.体内研究Cladribine(10μg/kg;i.p.;3times/week;for2weeks)mayhavebenefitsinthetreatmentofischemia/reperfusioninjurytothebiochemicalandhistopathologicparameters[3].Cladribine(0.5mg/kg;i.p.;daily;for60days)increasesamyloidbetapeptidegenerationandplaqueburdeninAPdE9mice[4].CladribineexhibitsCmax(rat4.9ng/mL)followingintra-arterialinjection[5].CladribineexhibitsCmax(rat1.1ng/mL)followingsubcutaneousinjection[5].Cladribineexhibitseliminationhalf-lives(rat3.5h)andplasmaclearance(rat2.8L/h/kg)followingintra-arterialinjection[5].Cladribineexhibitseliminationhalf-lives(rat4.5h)andplasmaclearance(rat2.3L/h/kg)followingsubcutaneousinjection[5].Cladribineadministrationwiths.c.injectionmayproducemorefavourablepharmacokineticprofilesthani.a.injectionfollowingasingledose[5].AnimalModel:MaleSprague-Dawleyrats,ischemicinjurymodel[3]Dosage:10μg/kgAdministration:Intraperitonealinjection,3times/week,for2weeksResult:MightincreaseexpressionofSphk1andconsecutivelySphK1suppressedHIF-1α.3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MaleSpragueDawleyrats(350-450g)[5]Dosage:2mg/kgfors.c.,1mg/kgfori.a.(PharmacokineticAnalysis)Administration:Subcutaneousinjection,intra-arterialResult:Cmax(4.9ng/mLi.a.;1.1ng/mLs.c.),T1/2β(3.5hi.a.;4.5s.c.).户使⽤本产品发表的科研⽂献•Molecules.2018Mar23;23(4).pii:E736.•ChemPharmBull(Tokyo).2017Aug1;65(8):768-775.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LinyanXu,etal.CladribineInducesATF4MediatedApoptosisandSynergizeswithSAHAinDiffuseLargeB-CellLymphomaCells.IntJMedSci.2020;17(10):1375–1384.[2].JianMa,etal.TherapeuticpotentialofcladribineincombinationwithSTAT3inhibitoragainstmultiplemyeloma.BMCCancer.2011Jun16;11:255.[3].YoungSeopChang,etal.MP28-10COMBINEDEFFECTSOFMELATONINANDCLADRIBINEONAPOPTOSISINISCHEMIA/REPERFUSIONINJURYINRATBLADDER.THEJOURNALOFUROLOGY.April2016.195(4S):e375.[4].CrystalDHayes,etal.Chroniccladribineadministrationincreasesamyloidbetapeptidegenerationandplaqueburdeninmice.PLoSOne.2012;7(10):e45841.[5].Yeung,P.K.F.,etal.PharmacokineticsofCladribineinaRatModelFollowingSubcutaneousandIntr