Trastuzumab-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemETrastuzumabCat.No.:HY-P9907CASNo.:180288-69-1分?式:C????H?????N????O????S??分?量:145531.5作?靶點:EGFR作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertBIOLOGICALACTIVITY?物活性Trastuzumab?種?化單克隆抗體，其以?親和?與HER2選擇性結(jié)合。Trastuzumab可?于HER2陽性轉(zhuǎn)移性乳腺癌和HER2陽性胃癌的研究。IC50&TargetHER2體外研究TreatmentofHER2-overexpressingbreastcancercelllineswithTrastuzumabresultsininductionofp27KIP1andtheRb-relatedprotein,p130,whichinturnsignificantlyreducesthenumberofcellsundergoingS-phase.AnumberofotherphenotypicchangesareobservedinvitroasaconsequenceofTrastuzumabbindingtoHER2-overexpressingcells.InteractionofTrastuzumabwiththehumanimmunesystemviaitshumanimmunoglobulinG1Fcdomainmaypotentiateitsantitumoractivities.invitrostudiesdemonstratethatTrastuzumabisveryeffectiveinmediatingantibody-dependentcell-mediatedcytotoxicityagainstHER2-overexpressingtumortargets[1].Trastuzumabconsistsoftwoantigen-specificsitesthatbindtothejuxtamembraneportionoftheextracellulardomainoftheHER2receptorandthatpreventtheactivationofitsintracellulartyrosinekinase.Trastuzumabrecruitsimmuneeffectorcellsthatareresponsibleforantibody-dependentcytotoxicity[2].ThepresenceofTrastuzumabIgGsignificantlyincreaseskillingofallbreastcancercelllines.TheADCCactivityofPBMCsevokedbyTrastuzumabisequallystrongagainstTrastuzumab-sensitive(SKBR-3)orTrastuzumab-resistant(JIMT-1)breastcancercells,withdose-dependentcelldeathreaching50–60%killingataneffector/targetratioof60:1[3].體內(nèi)研究Trastuzumabtreatmentofmousexenograftmodelsresultsinmarkedsuppressionoftumorgrowth.Whengivenincombinationwithstandardcytotoxicchemotherapeuticagents,Trastuzumabtreatmentgenerallyresultsinstatisticallysuperiorantitumorefficacycomparedwitheitheragentgivenalone[1].TrastuzumabcausesasignificantgrowthinhibitionoftheoutgrowthofmacroscopicJIMT-1xenografttumorsinbothnudeandSCIDmice[3].1/3www.MedChemEwww.MedChemEPROTOCOLCellAssay[3]TheeffectsofTrastuzumabandTrastuzumab-F(ab′)2onthegrowthofJIMT-1,SKBR-3,andBT-474cellsareevaluatedusingtheAlamarBluemethod.Exponentiallygrowingcellsareharvestedandplatedinsinglewellsofa96-wellflat-bottomedtissuecultureplateatdefineddensities,rangingfrom4,500-8,000cellsperwelldependingonthecellline.Afterovernightculture,theregularmediumisexchangedtomediumcontaining0,1,10,or100μg/mLTrastuzumaborTrastuzumab-F(ab′)2.Cellviabilityistestedafter72hoftreatment.Fluorescenceisdetectedatanexcitationof544nm,andemissionisdetectedat590nm[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalTrastuzumabandTrastuzumab-F(ab′)2aregivenatadoseof5and25μg/g,respectively,byweeklyi.p.Administration[3]injection.ThefivetimesgreateramountofadministeredF(ab′)2ischosenbasedonthedifferenthalf-livesofIgGandF(ab′)F(ab′)2.Controlmicearetreatedwithweeklyi.p.injectionof100μLphysiologicsaline(saline).AnimalsareeuthanizedbyCO2inhalation[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?SignalTransductTargetTher.2020Sep14;5(1):200.?NatCommun.2020Feb26;11(1):1049.?CancerLett.2020Apr10;475:53-64.?Elife.2019Jun7;8:e46983.?JExpClinCancerRes.2019May22;38(1):214.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SliwkowskiMX,etal.Nonclinicalstudiesaddressingthemechanismofactionoftrastuzumab.SeminOncol.1999Aug;26(4Suppl12):60-70.[2].HudisCA,etal.Trastuzumab--mechanismofactionanduseinclinicalpractice.NEnglJMed.2007Jul5;357(1):39-51.[3].BarokM,etal.Trastuzumabcausesantibody-dependentcellularcytotoxicity-mediatedgrowthinhibitionofsubmacroscopicJIMT-1breastcancerxenograftsdespiteintrinsicdrugresistance.MolCancerTher.2007Jul;6(7):2065-72.McePdfHeight2/3www.MedChemEwww.MedChemE關(guān)注MCE中國公眾號，

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