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Multi-kinaseinhibitor.ExhibitsinhibitoryactivityagainstChk2,KDR,FGFR,AuroraAkinaseandCdk2(IC50valuesare24,34,50,58and88nMrespectively).AlsobindsVEGFR-2,FGFR1andPDGFRβ(Kdvaluesare0.015,0.061and0.088μMrespectively).Displaysantiproliferativeactivityinvitro;inhibitsmitosisandangiogenesis.Orallybioavailable.
R1530isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight356.78.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Liuetal(2013)Discoveryofahighlypotent,orallyactivemitosis/angiogenesisinhibitorR1530forthetreatmentofsolidtumors.ACSMed.Chem.Lett.4259PMID:
Tovaretal(2010)Small-moleculeinducerofcancercellpolyploidypromotesapoptosisorsenescence:implicationsfortherapy.CellCycle93364PMID:20814247
Keywords:R1530,supplier,R1530,multi-RTK,inhibitors,inhibits,receptor,tyrosine,kinases,Chk2,KDR,FGFR,Aurora,A,Cdk2,VEGFR-2,FGFR1,PDGFRb,PDGFRbeta,PDGFRβ,angiogenesis,antiangiogenics,Other,RTKs,Antiangiogenics,Other,RTKs,TocrisBioscience
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