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Potent,selectiveinhibitorofVEGFR-2tyrosinekinase(IC50=0.9nM).Displayssomeinhibitoryactivitytowardsc-Kit,PDGFRαandFGFR-2(IC50valuesrangefrom40to170nM)butishighlyselectiveoverotherreceptortyrosinekinases(IC50>10000nMforFGFR-2,EGFRandHGFR).InhibitsVEGF-stimulatedproliferationofhumanumbilicalveinendothelialcells(HUVEC)andinhibitstumorgrowthinvivo;antiangiogenic.
Ki8751isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight469.41.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Kuboetal(2005)NovelpotentorallyactiveselectiveVEGFR-2tyrosinekinaseinhibitors:synthesis,structure-activityrelationships,andantitumouractivitiesofN-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.J.Med.Chem.481359PMID:15743179
Keywords:Ki8751,supplier,Potent,selective,VEGFR-2,inhibitors,inhibits,Vascular,Endothelial,Growth,Factors,Receptors,KDR,Flt,Receptor,Tyrosine,Kinases,RTKs,Ki8751,VEGFR,VEGFR,TocrisBioscience
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