Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECapecitabineCat.No.:HY-B0016CASNo.:154361-50-9分?式:C??H??FN?O?分?量:359.35作?靶點:DNA/RNASynthesis;NucleosideAntimetabolite/Analog;Apoptosis作?通路:CellCycle/DNADamage;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(695.70mM;Needultrasonic)H2O:≥33.33mg/mL(92.75mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7828mL13.9140mL27.8280mL5mM0.5566mL2.7828mL5.5656mL10mM0.2783mL1.3914mL2.7828mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?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：(為保證實驗結(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)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.79mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.79mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.79mM);Clearsolution4.請依序添加每種溶劑：PBSSolubility:25mg/mL(69.57mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Capecitabine?種可?于?服的前藥，可由胸苷磷酸化酶催化轉(zhuǎn)變?yōu)槠浠钚源x物Fluorouracil(FU)。IC50&TargetDNA/RNASynthesis[1]體外研究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].體內(nèi)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?邊的抑制劑?師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.戶使?本產(chǎn)品發(fā)表的科研?獻?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.