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商品描述
- Vatalanibisapotent,selective,orallyactiveinhibitoroftheVEGFRtyrosinekinasesVEGFR-1(Flt-1,IC50=77nM)andVEGFR-2(FLK-1/KDR,IC50=37nM),withslightlyhigherpotencyagainstthelatter.Athigherconcentrations,othertyrosinekinasesarealsoinhibited,includingPDGFR-β(IC50=580nM),c-KIT(IC50=730nM),FLT-4(IC50=660nM)andc-FMS(IC50=1.4µM).Ontheotherhand,vatalanibisnotactiveagainsttheEGFR,c-SRC,v-ABL,andproteinkinaseCα(IC50>10µM).Wood,J.M.,etal."PTK787/ZK222584,aNovelandPotentInhibitorofVascularEndothelialGrowthFactorReceptorTyrosineKinases,ImpairsVascularEndothelialGrowthFactor-inducedResponsesandTumorGrowthafterOralAdmiNISTration."CancerRes.60:2178-2189(2000).
- Vatalanibdose-dependentlyinhibitsproliferationofMMcellsandpatientcells(IC50=1-5µM),whicharebothsensitiveandresistanttoconventionaltherapy.VatalanibincreasestheinhibitoryeffectofdexamethasoneongrowthofMMcellsandcandecreasetheprotectiveeffectofinterleukin6(IL-6)againstdexamethasone-inducedapoptosis.Vatalanib(1µM)alsoinhibitsVEGF-inducedmigrationofMMcellsacrossanextracellularmatrix.Importantly,vatalanibalsoblockstheincreasedMMcellproliferationandincreasedIL-6andVEGFsecretioninculturesofMMcellsadherenttobonemarrowstemcells.Lin,B.,etal."ThevascularendothelialgrowthfactorreceptortyrosinekinaseinhibitorPTK787/ZK222584inhibitsgrowthandmigrationofmultiplemyelomacellsinthebonemarrowmicroenvironment."CancerRes.62:5019-5026(2002).
- VatalanibinhibitedVEGF-inducedphosphorylation(IC50"sof17nMand34nMforHUVECsandCHOcells,respectively),blockedthymidineincorporationinducedbyVEGFinHUVECs(IC50=7.1nM),preventedVEGF-inducedHUVECmigrationdosedependently(IC50=58nM),andinhibitedtumorcellproliferationwithanIC50of17µMand18µMforA431andDU145cells,respectivelyandsproutformationinrataortas(IC50=675nM).Wood,J.M.,etal."PTK787/ZK222584,aNovelandPotentInhibitorofVascularEndothelialGrowthFactorReceptorTyrosineKinases,ImpairsVascularEndothelialGrowthFactor-inducedResponsesandTumorGrowthafterOralAdministration."CancerRes.60:2178-2189(2000).
- Soldforlaboratoryormanufacturingpurposesonly;notforhuman,medical,veterinary,food,orhouseholduse.
- ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanADIanpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
- Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.
RelatedTerms:
[CGP-79787][PTK787][ZK222584]M.W.419.73
C20H15ClN4•2HCl
[212141-51-0]
M.I.14:9939