Capecitabine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECapecitabineCat.No.:HY-B0016CASNo.:154361-50-9分⼦式:C₁₅H₂₂FN₃O₆分⼦量:359.35作⽤靶点:DNA/RNASynthesis;NucleosideAntimetabolite/Analog;Apoptosis作⽤通路:CellCycle/DNADamage;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(695.70mM;Needultrasonic)H2O:≥33.33mg/mL(92.75mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7828mL13.9140mL27.8280mL5mM0.5566mL2.7828mL5.5656mL10mM0.2783mL1.3914mL2.7828mL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。-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:≥2.08mg/mL(5.79mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.79mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.79mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:25mg/mL(69.57mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Capecitabine⼀种可⽤于⼝服的前药，可由胸苷磷酸化酶催化转变为其活性代谢物Fluorouracil(FU)。IC50&TargetDNA/RNASynthesis[1]体外研究Capecitabineisananti-cancerchemotherapydrug.Itisclassifiedasanantimetabolite.Capecitabineisconvertedinto5′-deoxy-5-fluorocytidine(5′DFCR),5′-deoxy-5-fluorouridine(5′DFUR)and5-FUbycarboxylesterases(CES1and2),cytidinedeaminase(CDD),andthymidinephosphorylase(TP),inbothliverandtumour.Capecitabineinducesasignificantcytotoxiceffectinvitroonlyathighconcentrations.MeanIC50valuesvaryfrom860μMinCOLO205cellsto6000μMinHCT8cells[2].体内研究Apharmacokinetic/pharmacodynamicstudyiscarriedoutinmicebearingHCT116xenograftsreceiving0.52and2.1mmol/kg/dofCapecitabinebyoralgavage.Capecitabineadministeredat0.52mmol/kg/dayinducespartialcontrolofHCT116xenograftstumourgrowth:growthrate=7.5±0.5onday21.Capecitabine2.1mmol/kg/dayachievescompletecontroloftumorgrowthduringthetreatmentperiod:growthrate=1±0.2onday21[2].PROTOCOLCellAssay[2]HCT116,HCT8,HCT15,HT29,SW620andCOLO205humancoloncancercellsareused.Cellsareplatedonday1in96-wellplatesatadensityof2500cells/wellforHCT116,3500cells/wellforHCT8andHT29,5000cells/wellforHCT15,6000cells/wellforSW620and7000cells/wellsforCOLO205inavolumeof150μL/well.Allcelllinesaretreatedonday2withincreasingconcentrationsofCapecitabine(0.1-10mM),5′DFCR(10nM-100μM),5′DFUR(2.5-500μM)or5-FU(0.5-250μM)for24h.Afterdrugexposure,cellsarewashedoncewithcoldPBSandplacedin200μLofdrug-freemediumfor72haftertheendofdrugexposure.ThecellsarethenfixedwithtrichloroaceticacidandstainedwithsulforhodamineB.Opticaldensitiesaremeasuredat540nmwithaBiohitBP-800.Theresultsarebasedonthreeindependentexperimentsperformedintriplicate[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[2]Administration[2]Six-week-oldC57/Bl6Nu/Numiceareused.BilateralHCT116xenograftsareobtainedbysubcutaneous2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEinjectionof107cells/flank.AnimalsbearingHCT116xenograftsaretreatedwithvehicleorCapecitabine0.52or2.1mmol/kg(563and2250mg/m2,respectively)givenoncedailyfor5consecutivedays/weekbyoralgavagefor3weeks(days0-4,7-11,14-18).Animalsareculledonday0at15,30min,1,2,4,8and24h,andpriortoplannedtreatmentondays7and14afterthestartoftreatment.Threeanimalspertime-pointareanalysed.Atthetimeofcollection,bloodiscollectedinheparin,andplasmaisolatedandstoredat−80°C.TheliverisremovedimmediatelyandstoredinRNAlatersolution.Tumoursaremacro-dissectedtoremovefibrotictissueandbloodvesselsandsnap-frozeninliquidnitrogen.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•JAdvRes.12June2021.•CancerLett.2020Apr28;476:67-74.•CellDeathDiscov.2022May2;8(1):238.•ActaPharmacolSin.2021Jan;42(1):108-114.•FrontOncol.2021Jul13;11:704042.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PharmDCM,etal.Capecitabine:Areview.ClinicalTherapeutics.2005Jan;27(1):23-44.[2].GuichardSM,etal.Geneexpressionpredictsdifferentialcapecitabinemetabolism,impactingonbothpharmacokineticsandantitumouractivity.