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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Trametinib（同义词：GSK1120212；JTP-74057）/HY-10999/10mM*1mL二甲基亚砜
商品详细Medchemexpress/Trametinib（同义词：GSK1120212；JTP-74057）/HY-10999/10mM*1mL二甲基亚砜
Medchemexpress/Trametinib（同义词：GSK1120212；JTP-74057）/HY-10999/10mM*1mL二甲基亚砜
Medchemexpress/Trametinib（同义词：GSK1120212；JTP-74057）/HY-10999/10mM*1mL二甲基亚砜
商品编号： HY-10999-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
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
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商品介绍
TrametinibisapotentMEK1/2inhibitorthatspecificallyinhibitsMEK1/2,withanIC50valueofabout2nM.

CustomerValidation

  • •CancerDiscov.2015Sep;5(9):960-71.
  • •CancerDiscov.2012Oct;2(10):934-47.
  • •ClinCancerRes.2014Nov1;20(21):5483-95.
  • •StemCellReports.2017Nov23.pii:S2213-6711(17)30483-6.
  • •StemCellReports.2016Jan12;6(1):74-84.
  • •CancerLett.2017Aug18;408:43-54.
  • •MolCancerTher.2016Aug;15(8):1859-69.
  • •Oncotarget.2017Feb28;8(9):14835-14846.
  • •Oncotarget.2015Oct13;6(31):31313-22.
  • •SciRep.2017Mar28;7:45332.
  • •SciRep.2016Oct19;6:35531.
  • •JCellBiochem.2016Jun;117(6):1340-51.
  • •BiochemBiophysResCommun.2017Nov29.pii:S0006-291X(17)32354-9.
  • •OncolLett.September28,2017.
  • •AmJDigestDis.2015;2(2):95-99.
  • •JClinToxicol.2014October4,4:5.
  • •JClinToxicol.4:212.
  • •HarvardMedicalSchoolLINCSLIBRARY
Description

TrametinibisapotentMEK1/2inhibitorthatspecificallyinhibitsMEK1/2,withanIC50valueofabout2nM.

IC50&Target

IC50:2nM(MEK1/2)[1]

InVitro

Trametinib(0.1-100nM)blockstumornecrosisfactor-αandinterleukin-6productionfromperipheralbloodmononuclearcells(PBMCs).Trametinib(JTP-74057)inhibitsthegrowthof9outof10humancolorectalcancercelllines,andtheyshowscell-cyclearrestattheG1phaseafterdrugtratment[1].ThecombinationofGSK2118436andTrametinib(GSK1120212)effectivelyinhibitscellgrowth,decreasesERKphosphorylation,decreasescyclinD1protein,andincreasesp27(kip1)proteinintheresistantclones[2].

InVivo

Adjuvant-inducedarthritis(AIA)andtypeIIcollageninducedarthritis(CIA)developmentaresuppressedalmostcompletelyby0.1mg/kgofJTP-74057or10mg/kgofLeflunomide.IntheCIA,JTP-74057suppressescollagen-reactiveT-cellproliferationexvivo[1].Trametinib(0.3mg/kg,1mg/kg,p.o.)effectiveininhibitingtheHT-29xenograftgrowthinanudemousexenograftmodel[2].

ClinicalTrial
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References

  • [1].YamaguchiT,etal.SuppressiveeffectofanorallyactiveMEK1/2inhibitorintwodifferentanimalmodelsforrheumatoidarthritis:acomparisonwithleflunomide.InflammRes,2012,61(5),445-454.

    [2].YamaguchiT,etal.AntitumoractivitiesofJTP-74057(GSK1120212),anovelMEK1/2inhibitor,oncolorectalcancercelllinesinvitroandinvivo.IntJOncol,2011,39(1),23-31.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.6250mL8.1249mL16.2499mL
5mM0.3250mL1.6250mL3.2500mL
10mM0.1625mL0.8125mL1.6250mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[2]

Thenonphosphorylatedmyelinbasicprotein(MBP)iscoatedontoanELISAplate,andtheactiveformofB-Raf/c-RafismixedwithunphosphorylatedMEK1/MEK2andERK2in10µMATPand12.5mMMgCl2containingMOPSbufferinthepresenceofvariousconcentrationsofTrametinib(JTP-74057).ThephosphorylationofMBPisdetectedbytheanti-phosphoMBPantibody.Kinaseinhibitoryactivitiesagainstatotalof99kinasesaretestedat10µMATP[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[2]

Trametinib(JTP-74057)isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse[2].

CellsaretreatedwithvariousconcentrationsofTrametinib(JTP-74057)in100mmdishesfor3or4days.Bothfloatingandadherentcellsarecollectedandfixedwith70%ethanol.AfterwashingwithPBS,thecellsaresUSPendedin100µL/mLRNaseand25µL/mLpropidiumiodide(PI)andincubatedat37°Cfor30mininthedark.TheDNAcontentofeachsinglecellisdeterminedusingtheflowcytometerCytomicsFC500orGuavaEasyCyteplus[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[2]

Trametinibisdissolvedin10%CremophorEL-10%PEG400(Mice)[2].

Mice[2]
FemaleBALB/c-nu/numiceareused.Onday0,HT-29cellsorCOLO205cellssuspendedinice-coldHBSS(-)areinoculatedsubcutaneouslyintotherightflankofthemiceat5×106cells/100µL/siteor1×106cells/100µL/site,respectively.Theaceticacid-solvatedformofTrametinib(JTP-74057,0.3mg/kg,1mg/kg)isdissolvedin10%CremophorEL-10%PEG400andisadministeredorallyoncedailyfor14daysfromthedaywhenthemeantumorvolumereached100mm3.Thetumorlength[L(mm)]andwidth[W(mm)]aremeasuredusingamicrogaugetwiceaweekaftercommencementofdosing,andthetumorvolumeiscalculatedusingthefollowingformula:tumorvolume(mm3)=L×W×W/2.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].YamaguchiT,etal.SuppressiveeffectofanorallyactiveMEK1/2inhibitorintwodifferentanimalmodelsforrheumatoidarthritis:acomparisonwithleflunomide.InflammRes,2012,61(5),445-454.

    [2].YamaguchiT,etal.AntitumoractivitiesofJTP-74057(GSK1120212),anovelMEK1/2inhibitor,oncolorectalcancercelllinesinvitroandinvivo.IntJOncol,2011,39(1),23-31.

MolecularWeight

615.39

Formula

C₂₆H₂₃FIN₅O₄

CASNo.

871700-17-3

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:99.37%