Methotrexate-Amethopterin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMethotrexateCat.No.:HY-14519CASNo.:59-05-2Synonyms:Amethopterin;CL14377;WR19039分⼦式:C₂₀H₂₂N₈O₅分⼦量:454.44作⽤靶点:Antifolate;DNA/RNASynthesis;ADCCytotoxin;Apoptosis;Bacterial作⽤通路:CellCycle/DNADamage;Antibody-drugConjugate/ADCRelated;Apoptosis;Anti-infection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(110.03mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2005mL11.0026mL22.0051mL5mM0.4401mL2.2005mL4.4010mL10mM0.2201mL1.1003mL2.2005mL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(5.50mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.50mM);Clearsolution3.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(5.50mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.50mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Methotrexate(Amethopterin)⼀种抗代谢(antimetabolite)和抗叶酸剂(antifolate)，可抑制⼆氢叶酸还原酶，从⽽防⽌叶酸转化为四氢叶酸并抑制DNA合成。Methotrexate也⼀种免疫抑制剂和抗肿瘤剂，⽤于类风湿关节炎和研究多种癌症(如急性淋巴细胞⽩⾎病)。IC50&TargetTraditionalCytotoxicAgents体内研究Methotrexate(Amethopterin)reducesthymusandspleenindicesofmice.Methotrexatemarkedlydecreaseswhitebloodcells,thymicandspleniclymphocytesatdose≥5mg/kg.However,thereisasignificantdifferencebetweenthetreatmentpluscontrolgroupandthemodelgroup(p[2].Methotrexate(MTX)(2mg/kg;i.p.;onceinaweekfor5weeks)iseffectiveinFreund'scompleteadjuvant-inducedarthritis.ThecombinationofMethotrexate(1mg/kg;i.p.;onceinaweekfor5weeks)andCurcumin(30mg/kgand100mg/kg,thriceaweekfor5weeks;i.p.)showsasignificantanti-arthriticactionandprotectionfromhematologicaltoxicity[4].PROTOCOLCellAssay[1]Eachcelllineisstudiedingrowthinhibitionexperimentsusing96-wellmicrotiterplates.Asantifolsarescheduledependent,preliminaryexperimentsareaimedatdefiningthelongestdurationofexposurethatwouldallowforcontinuouslogarithmicphasegrowthofcellswithoutchangingoftheculturemediawhilemaintainingalinearrelationshipbetweenSRBopticaldensityandcellnumber.Twenty-fourhoursaftercellplating,thecelllinesareexposedtotheantifolfor120h(threereplicatesperexperiment).Toensurethatacompletesigmoidalsurvival-concentrationcurvecouldbeobserved,thefollowingdrugconcentrationsarestudied:Methotrexate(0.002-5μM),AMT(0.0001-1μM),PXD(0.0003-10μM),TLX(0.0002-0.5μM).Experimentsarerepeatedatleasttwice[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[2]Administration[2]ThecombinationofbioactivephytochemicalsisadministeredoneweekpriortotheMethotrexateexposure.TreatmentgroupI:micearegivenacombinationofgreenteapolyphenolsandeleutherosidesfromSiberianginseng(0.2mL/10g,i.g.oncedaily)for15days,andasingledoseofMethotrexate(2mg/kg,i.p.oncedaily)isaddedonthe8thday.TreatmentgroupII:micearegivenacombinationofgrapeseed2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEproanthocyanidinsandeleutherosidesfromSiberianginsengfor15days,andMethotrexateisadministeredonthe8thdayinasimilarmanner.Modelgroup:animalsreceiveddistilledwaterinsteadofbioactivephytochemicalscombinationsfor15daysandthesameMethotrexateprotocolappliedtothisgrouponthe8thday.Controlgroup:micearegivendistilledwaterthrough15daysandphysiologicalsalineinsteadofMethotrexateisadministeredonthe8thdayinasimilarmanner.Twelvehoursafterthefinaldoses,theanimalsareeuthanizedbycervicaldislocation.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Small.2022Jul;18(30):e2202337.•EMBOMolMed.2022Feb17;e14552.•JPharmAnal.7August2022.•CellDeathDis.2020Nov12;11(11):976.•ActaPharmacolSin.2021Jan;42(1):108-114.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TianH,etal.Understandingthemechanismsofactionofmethotrexate:implicationsforthetreatmentofrheumatoidarthritis.BullNYUHospJtDis.2007;65(3):168-73.[2].SwierkotJ,etal.Methotrexateinrheumatoidarthritis.PharmacolRep.2006Jul-Aug;58(4):473-92.[3].EhabTousson,etal.TheEffectofL-carnitineonAmethopterin-inducedToxicityinRatLargeIntestine.[4].BanjiD,etal.EvaluationoftheconcomitantuseofmethotrexateandcurcuminonFreund'scompleteadjuvant-inducedarthritisandhematologicalin