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《The Microtubule Depolymerizing Agent CYT997 CausesExtensive Ablation of Tumor Vasculature In Vivo□S微管解聚劑cyt997原因 腫瘤血管在體內(nèi)□廣泛消融》由會(huì)員上傳分享，免費(fèi)在線閱讀，更多相關(guān)內(nèi)容在學(xué)術(shù)論文-天天文庫。
1、Supplementalmaterialtothisarticlecanbefoundat:http://jpet.aspetjournals.org/content/suppl/2011/09/14/jpet.111.186965.DC10022-3565/11/3393-799–806$25.00THEJOURNALOFPHARMACOLOGYANDEXPERIMENTALTHERAPEUTICSVol.339,No.3Copyright?2011byTheAmericanSocietyforPharm
2、acologyandExperimentalTherapeutics186965/3732157JPET339:799–806,2011PrintedinU.S.A.TheMicrotubuleDepolymerizingAgentCYT997CausesExtensiveAblationofTumorVasculatureInVivo□SChristopherJ.Burns,EmmanuelleFantino,AndrewK.Powell,StevenD.Shnyder,PatriciaA.Cooper,
3、StuartNelson,ChristopherChristophi,CathyMalcontenti-Wilson,ValentinaDubljevic,MichaelF.Harte,MaxJoffe,IanD.Phillips,DavidSegal,AndrewF.Wilks,andGreggD.SmithYMBioSciencesAustralia,Frankston,Victoria,Australia(C.J.B.,E.F.,A.K.P.,V.D.,M.F.H.,M.J.,I.D.P.,D.S.,
4、A.F.W.,G.D.S.);InstituteofCancerTherapeutics,UniversityofBradford,Bradford,WestYorkshire,UnitedKingdom(S.D.S.,P.A.C.,S.N.);andDownloadedfromDepartmentofSurgery,UniversityofMelbourne,AustinHealth,Heidelberg,Victoria,Australia(C.C.,C.M.-W.)ReceivedAugust14,2
5、011;acceptedSeptember12,2011ABSTRACTjpet.aspetjournals.orgTheorallyactivemicrotubule-disruptingagent(S)-1-ethyl-3-(2-icalchangesat100nM,includingmembraneblebbing.Usingthemethoxy-4-(5-methyl-4-((1-(pyridin-3-yl)butyl)amino)pyrimidin-2-methodofcorrosioncasti
6、ngvisualizedwithscanningelectronyl)phenyl)urea(CYT997),reportedpreviouslybyus(BioorgMedmicroscopy,asingledoseofCYT997(7.5mg/kgi.p.)inameta-ChemLett19:4639–4642,2009;MolCancerTher8:3036–3045,staticcancermodelwasshowntocausedestructionoftumor2009),ispotently
7、cytotoxictoavarietyofcancercelllinesinvitromicrovasculatureinmetastaticlesions.Furthermore,repeatdos-andshowsantitumoractivityinvivo.InadditiontoitscytotoxicingofCYT997at10mg/kgandabove(intraperitoneally,b.i.d.)wasactivity,CYT997possessesantivasculareffect
8、sontumorvascu-showntoeffectivelyinhibitdevelopmentoflivermetastases.Thelature.Tofurthercharacterizethevasculardisruptingactivityoftimeanddosedependenceoftheantivasculareffectswerestud-atASPETJournalsonAugust1
