Linifanib

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Linifanib
Linifanib skeletal.svg
Clinical data
ATC code
  • None
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.206.772
Chemical and physical data
Formula C17H15FN5O
Molar mass 375.41 g/mol
3D model (JSmol)
  (verify)

Linifanib (ABT-869) is a structurally novel, potent inhibitor of receptor tyrosine kinases (RTK), vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) with IC50 of 0.2, 2, 4, and 7 nM for human endothelial cells, PDGF receptor beta (PDGFR-β), KDR, and colony stimulating factor 1 receptor (CSF-1R), respectively. It has much less activity (IC50s > 1 μM) against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. In vivo linifanib is effective orally in mechanism-based murine models of VEGF-induced uterine edema (ED50 = 0.5 mg/kg) and corneal angiogenesis (>50%inhibition, 15 mg/kg).[1][2]

References[edit]

  1. ^ Albert, D. H.; Tapang, P.; Magoc, T. J.; Pease, L. J.; Reuter, D. R.; Wei, R. Q.; Li, J.; Guo, J.; Bousquet, P. F.; Ghoreishi-Haack, N. S.; Wang, B.; Bukofzer, G. T.; Wang, Y. C.; Stavropoulos, J. A.; Hartandi, K.; Niquette, A. L.; Soni, N.; Johnson, E. F.; McCall, J. O.; Bouska, J. J.; Luo, Y.; Donawho, C. K.; Dai, Y.; Marcotte, P. A.; Glaser, K. B.; Michaelides, M. R.; Davidsen, S. K. (2006). "Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor". Molecular Cancer Therapeutics. 5 (4): 995–1006. PMID 16648571. doi:10.1158/1535-7163.MCT-05-0410. 
  2. ^ Guo, J.; Marcotte, P. A.; McCall, J. O.; Dai, Y.; Pease, L. J.; Michaelides, M. R.; Davidsen, S. K.; Glaser, K. B. (2006). "Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors". Molecular Cancer Therapeutics. 5 (4): 1007–1013. PMID 16648572. doi:10.1158/1535-7163.MCT-05-0359.