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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Paclitaxel/HY-B0015/500mg
商品详细Medchemexpress/Paclitaxel/HY-B0015/500mg
Medchemexpress/Paclitaxel/HY-B0015/500mg
Medchemexpress/Paclitaxel/HY-B0015/500mg
商品编号： HY-B0015-10mM*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
电子邮箱： info@ebiomall.com
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商品介绍
Paclitaxelisapotentanticanceragentknowntopromotemicrotubule(MT) assembly,inhibitMTdepolymerization,andchangeMTdynamicsrequiredformitosisandcellproliferation.

CustomerValidation

  • •AmJCancerRes.2017Apr1;7(4):903-912.
  • •UniversidadedoPorto.2015-11-16.
  • •UniversidadedoPorto.Setembro/2015.
  • •HarvardMedicalSchoolLINCSLIBRARY
Description

Paclitaxelisapotentanticanceragentknowntopromotemicrotubule(MT) assembly,inhibitMTdepolymerization,andchangeMTdynamicsrequiredformitosisandcellproliferation.

IC50&Target

IC50:4nM(MT)

InVitro

Paclitaxelat0.1,0.5,and1μMreducestheproliferationandsurvivalofCCRF-HSB-2cellsinadose-dependentfashionandthattheIC50valueoftaxolisabout0.25μM[1].Paclitaxeldirectlyassociateswiththeendoplasmicreticulumtostimulatethereleaseofcalciumintothecytosol,contributingtotheinductionofapoptosis[2].

InVivo

InaSCIDmousexenograftmodel,lowdosemetronomicPaclitaxeltreatmentdecreaseslungdisseminationofEGI-1cellswithoutsignificantlyaffectingtheirlocaltumorgrowth[3].Lowdosesofpaclitaxelpromotlivermetastasisinmousexenografts,whichcorrelatswithchangesinestrogenmetabolisminthehostliver[4].Paclitaxel(2mg/kgpertreatment,blackcircles)inducesmechanicalhypersensitivityintheglabrousskinofthehindpaw[5].

ClinicalTrial
ViewMoreCollapse
References

  • [1].ParkSJ,etal.Taxolinducescaspase-10-dependentapoptosis.JBiolChem.2004Dec3;279(49):51057-67.Epub2004Sep27.

    [2].PanZ,etal.PaclitaxelattenuatesBcl-2resistancetoapoptosisinbreastcancercellsthroughanendoplasmicreticulum-mediatedcalciumreleaseinadosagedependentmanner.BiochemBiophysResCommun.2013Feb13.pii:S0006-291X(13)00259-3.

    [3].CadamuroM,etal.LowdosepaclitaxelreducesS100A4nuclearimporttoinhibitinvasionandhematogenousmetastasisofcholangiocarcinoma.CancerRes.2016Jun21.

    [4].LiQ,etal.Lowdosesofpaclitaxelenhancelivermetastasisofbreastcancercellsinthemousemodel.FEBSJ.2016Jun16.

    [5].YilmazE,etal.Sensoryneuronsubpopulation-specificdysregulationofintracellularcalciuminaratmodelofchemotherapy-inducedperipheralneuropathy.Neuroscience.2015Aug6;300:210-8.

    [6].JingC,etal.Lenvatinibenhancestheantitumoreffectsofpaclitaxelinanaplasticthyroidcancer.AmJCancerRes.2017Apr1;7(4):903-912.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.1711mL5.8554mL11.7108mL
5mM0.2342mL1.1711mL2.3422mL
10mM0.1171mL0.5855mL1.1711mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[1]

Todeterminewhichcaspasesareinvolvedinapoptosisinducedbytaxol,caspase-3inhibitor(DEVD-CHO),caspase-6inhibitor(Z-VEID-FMK),caspase-8inhibitor(Z-IETD-FMKorIETD-CHO),caspase-9inhibitors(Z-LEHD-FMKorLEHD-CHO),andcaspase-10inhibitor(Z-AEVD-FMK)areused.Thesecaspaseinhibitorsaredissolvedindimethylsulfoxide(Me2SO);thefinalconcentrationofMe2SOis0.1%.Cells(5×105)arepreincubatedinthepresenceorabsenceof100μM eachoftheseinhibitorsfor3hat37°Cthentreatedwithorwithout0.1,0.5,and1μM Paclitaxelfor48handprocessedforannexinVbindingassay.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[1]

1×104cellsareplatedin100μLofthegrowthmediuminthepresenceorabsenceofincreasingconcentrations(0.1-1μM)oftaxolin96-wellplatesandculturedat37°Cin5%CO2for12-48h.Thecellsarethenincubatedwith25μLofMTT(5mg/mL)at37°Cfor4h.Afterdissolvingthecrystalswith0.04 N HClinisopropanol,theplatesarereadinamicroplatereaderat570nm.Theconcentrationofdrugthatinhibitscellsurvivalby50%(IC50)isdeterminedfromcellsurvivalplots.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[5]

Paclitaxelisdissolvedat25mg/mLin1:1CremophorEL:ethanolandfreshlydiluted1:12.5in0.9%sterilesalinepriortoinjections.

Adult(250-320g)maleSprague-Dawleyratsareusedforallexperiments.Ratsarehousedtwopercageinatemperatureandhumiditycontrolled,ona12h:12hlight:darkschedulewithfoodandwateravailableadlibitum.OneweekfollowingtheDiIinjection,ratsareanesthetizedwithisofluoraneandinjectedintothetailveinwith2mg/kgpaclitaxeloritsvehicle(1:1:23,cremophorEL:ethanol:0.9%saline).Thetailveininjectionisrepeatedthreemoretimeseveryotherdayforatotaloffourinjections.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].ParkSJ,etal.Taxolinducescaspase-10-dependentapoptosis.JBiolChem.2004Dec3;279(49):51057-67.Epub2004Sep27.

    [2].PanZ,etal.PaclitaxelattenuatesBcl-2resistancetoapoptosisinbreastcancercellsthroughanendoplasmicreticulum-mediatedcalciumreleaseinadosagedependentmanner.BiochemBiophysResCommun.2013Feb13.pii:S0006-291X(13)00259-3.

    [3].CadamuroM,etal.LowdosepaclitaxelreducesS100A4nuclearimporttoinhibitinvasionandhematogenousmetastasisofcholangiocarcinoma.CancerRes.2016Jun21.

    [4].LiQ,etal.Lowdosesofpaclitaxelenhancelivermetastasisofbreastcancercellsinthemousemodel.FEBSJ.2016Jun16.

    [5].YilmazE,etal.Sensoryneuronsubpopulation-specificdysregulationofintracellularcalciuminaratmodelofchemotherapy-inducedperipheralneuropathy.Neuroscience.2015Aug6;300:210-8.

    [6].JingC,etal.Lenvatinibenhancestheantitumoreffectsofpaclitaxelinanaplasticthyroidcancer.AmJCancerRes.2017Apr1;7(4):903-912.

MolecularWeight

853.91

Formula

C₄₇H₅₁NO₁₄

CASNo.

33069-62-4

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥31mg/mL;H2O:<0.1="">

Paclitaxelisdissolvedat20mg/mLinDMSOandfreshlydiluted(1:1-1:200)asasUSPensionwithPBS.
PaclitaxelisdissolvedinDMSO,aliquotedandstoredat-80°Cuntilfurtheruse.ThesamevolumeofDMSOisusedasthevehiclecontrol[6].

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

References

  • [1].ParkSJ,etal.Taxolinducescaspase-10-dependentapoptosis.JBiolChem.2004Dec3;279(49):51057-67.Epub2004Sep27.

    [2].PanZ,etal.PaclitaxelattenuatesBcl-2resistancetoapoptosisinbreastcancercellsthroughanendoplasmicreticulum-mediatedcalciumreleaseinadosagedependentmanner.BiochemBiophysResCommun.2013Feb13.pii:S0006-291X(13)00259-3.

    [3].CadamuroM,etal.LowdosepaclitaxelreducesS100A4nuclearimporttoinhibitinvasionandhematogenousmetastasisofcholangiocarcinoma.CancerRes.2016Jun21.

    [4].LiQ,etal.Lowdosesofpaclitaxelenhancelivermetastasisofbreastcancercellsinthemousemodel.FEBSJ.2016Jun16.

    [5].YilmazE,etal.Sensoryneuronsubpopulation-specificdysregulationofintracellularcalciuminaratmodelofchemotherapy-inducedperipheralneuropathy.Neuroscience.2015Aug6;300:210-8.

    [6].JingC,etal.Lenvatinibenhancestheantitumoreffectsofpaclitaxelinanaplasticthyroidcancer.AmJCancerRes.2017Apr1;7(4):903-912.

Purity:99.60%