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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/丝裂霉素C（同义词：阿米替因）/HY-13316/10mg
商品详细Medchemexpress/丝裂霉素C（同义词：阿米替因）/HY-13316/10mg
Medchemexpress/丝裂霉素C（同义词：阿米替因）/HY-13316/10mg
Medchemexpress/丝裂霉素C（同义词：阿米替因）/HY-13316/10mg
商品编号： HY-13316-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1100.00
美元价： 660.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
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商品介绍
MitomycinCisaDNA-damagingagentandsmall-moleculeinhibitoreffectivelysensitizecancercellstotumornecrosisfactor(TNF)-relatedapoptosis-inducingligand(TRAIL).

CustomerValidation

  • •JExpClinCancerRes.2016Nov7;35(1):173.
  • •SciRep.2017Jun30;7(1):4469.
  • •ExpCellRes.2016Feb15;341(2):157-65.
  • •BiomedPharmacother.2017Aug18;95:18-24.
  • •DrugsRD.2017Jun;17(2):297-304.
Description

MitomycinCisaDNA-damagingagentandsmall-moleculeinhibitoreffectivelysensitizecancercellstotumornecrosisfactor(TNF)-relatedapoptosis-inducingligand(TRAIL).

IC50&Target

DNAsynthesis[1]

InVitro

TheHCT116(p53-/-)cellsareminimallysensitivetoeitherMitomycinCorTRAILalone.However,surprisingly,combinationtreatmentwithMMCandTRAILdecreasescellviABIlitysignificantly.AlthoughMitomycinCandTRAILalonearemoderatelyeffective,MitomycinCsubstantiallyenhancestheeffectofTRAILonsuppressionofthecellproliferation.MitomycinCandTRAILtreatmentaloneinduces9.5%and35.0%apoptosis,respectively.However,combinationtreatmentwithMitomycinCandTRAILenhancesapoptosisto66.6%[1].MitomycinCisacytotoxicchemotherapeuticagentthatcausesDNAdamageintheformofDNAcross-linksaswellasavarietyofDNAmonoadductsandisknowntoinducep53[2].

InVivo

MicebearingxenograftedHCT116(p53-/-)colontumorsandHT-29colontumorsaretreatedwithMitomycinC(i.p.,1mg/kg)andTRAIL(i.v.,100μg)everyotherday.Animalsaretreatedwith10consecutivecyclesofthecombinationtherapyregimen.Thecombinationtherapysuppressestumorgrowthsignificantlyanddoesnotimpacttheweightofthemice,indicatingthatthetherapeuticcombinationofMitomycinCandTRAILiswell-toleratedandhasanti-tumoractivityinvivo[1].IntravesicalMitomycinCinstillationshasaneffectonbodyweightthatisnotobservedinnormal,NaClinstilledorEpirubicininstilledrats.After3consecutiveweeklyinstillationsof1mg/mLMitomycinCthereisalmostnoweightgain,whereasratsintheother3groupshasastatisticallysignificantweightgaincomparedwithMMCtreatedrats[3].

ClinicalTrial
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References

  • [1].ChengH,etal.MitomycinCpotentiatesTRAIL-inducedapoptosisthroughp53-independentupregulationofdeathreceptors:Evidencefortheroleofc-JunN-terminalkinaseactivation.CellCycle.2012Sep1;11(17):3312-23.

    [2].AbbasT,etal.Differentialactivationofp53bythevariousadductsofmitomycinC.JBiolChem.2002Oct25;277(43):40513-9.

    [3].MichielsenD,etal.MitomycinCandepirubicin:functionalbladderdamageinratsafterrepeatintravesicalinstillations.JUrol.2005Jun;173(6):2166-70.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.9911mL14.9553mL29.9106mL
5mM0.5982mL2.9911mL5.9821mL
10mM0.2991mL1.4955mL2.9911mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

MitomycinCisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[1].

ColonadenocarcinomaHCT116andHT-29humancoloncancercellsareused.TheCellTiter-GloLuminescentCellViabilityAssayisusedtomeasurecellviability,whichuseaunique,stableformofluciferasetomeasureATPasanindicatorofviablecells,andtheluminescentsignalproducedisproportionaltothenumberofviablecellspresentinculture.CellsarepretreatedwithMitomycinC(5μM)for12hor24h,andthenexposedtodifferentconcentrationsofTRAILfor12h.Anequalvolume(100μL)ofCellTiter-GloTMreagentisaddedandthesolutionismixedgentlyfor2minonanorbitalshaker.Mixtureisincubatedatroomtemperaturefor10mintoallowluminescentsignaltostabilize,andthenimagingisperformedusingtheXenogenIVISsystemtoquantifythecellviability[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[1][3]

MitomycinCispreparedinsaline(0.9%NaCl).

Mice[1]
Four-to6-wk-oldNCrnudemicearetreatedwithMitomycinC(1mg/kg)byintraperitonealinjectionfor24h,followedbyoneintravenousdoseofpurifiedrhTRAIL(100μg).Asanegativecontrol,asubsetofthemiceareinjected(i.p.andi.v.)withsaline(vehicle)atthesamefrequencyoftreatment.Animalsaretreatedfor3consecutiveweeks.Thetumorsizeismonitoredeveryweekusingcalipermeasurementsofthetumorvolume.
Rats[3]
YoungadultfemaleWistarratsatage13weekswithamedianweightof217g(range187to255)arerandomizedinto4groupsof10each,namelyanormalgroupwithnoinstillations,anNaCl0.9%orplacebogroupthatreceivedinstillationswiththesolventofthechemotherapeuticagents,anMitomycinC(1mg/mL)groupandanEpirubicin(1mg/mL)group.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].ChengH,etal.MitomycinCpotentiatesTRAIL-inducedapoptosisthroughp53-independentupregulationofdeathreceptors:Evidencefortheroleofc-JunN-terminalkinaseactivation.CellCycle.2012Sep1;11(17):3312-23.

    [2].AbbasT,etal.Differentialactivationofp53bythevariousadductsofmitomycinC.JBiolChem.2002Oct25;277(43):40513-9.

    [3].MichielsenD,etal.MitomycinCandepirubicin:functionalbladderdamageinratsafterrepeatintravesicalinstillations.JUrol.2005Jun;173(6):2166-70.

MolecularWeight

334.33

Formula

C₁₅H₁₈N₄O₅

CASNo.

50-07-7

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:30mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:98.51%