ProductDescription
XL184(Cabozantinib)isanoral,small-moleculeinhibitor,whichhaspotentactivitytowardVEGFR2(IC50=0.035nM)andMET(IC50=1.3nM),aswellasanumberofotherreceptortyrosinekinasesthathavealsobeenimplicatedintumorpathoBIOLOGy,includingRET,KIT,AXL,andFLT3[1].
Multiplereceptortyrosinekinases(RTKs)aresometimesactivatedinthesametumor.InhibitionofsingleRTKmayleadtocompensatorysignalingthatmaintainscellgrowth.Targetingmultiplekinasessimultaneouslymightovercomebothintrinsicandacquiredresistancetoantitumordrugs.XL184hasbeenshowntoinhibitphosphorylationofMETandVEGFR2,todisruptangiogenesisandcellularmigrationandinvasion,andtopromotetumorandendotheliacelldeath1.Inhibitionofc-MetwithXL184blocksself-renewalcapacityinpancreaticcancerstemcells(CSCs)[2].Inmousemodelsandpreclinicalstudies,XL184demonstratesrobustantiangiogenic,antitumor,andanti-invasiveeffects,dramaticallyalterstumorpathology,preventsthedevelopmentofmetastases,andreducestumorburden[1-3].
Technicalinformation:
ChemicalFormula: | C28H24FN3O5 | |
CAS#: | 849217-68-1 | |
MolecularWeight: | 501.51 | |
Purity: >98% | ||
Appearance: | White | |
ChemicalName: | N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | |
Solubility: | Upto22mMinDMSO | |
Synonyms: | XL184,XL-184,BMS-907351,BMS907351,Cabozantinib,Cometriq |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | YakesFM,etal.Cabozantinib(XL184),anovelMETandVEGFR2inhibitor,simultaneouslysuppressesmetastasis,angiogenesis,andtumorgrowth.MolCancerTher.2011.10(12):2298-308.PubmedID:21926191 |
2. | Herreros-VillanuevaM,etal.c-Metinpancreaticcancerstemcells:Therapeuticimplications.WorldJGastroenterol.2012.18(38):5321-3.PubmedID:23082047 |
3. | KurzrockR,etal.ActivityofXL184(Cabozantinib),anoraltyrosinekinaseinhibitor,inpatientswithmedullarythyroidcancer.JClinOncol.2011.29(19):2660-6.PubmedID:21606412 |
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