SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities.

@article{Alam2012SAR131675AP,
  title={SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities.},
  author={Antoine Alam and Isabelle Blanc and Genevi{\`e}ve Gueguen-Dorbes and Olivier Duclos and Jacques Bonnin and Pauline Barron and M. Laplace and Gaelle Morin and Florence Gaujarengues and Fr{\'e}d{\'e}rique Dol and Jean-Pascal H{\'e}rault and Paul Schaeffer and Pierre Savi and Françoise Bono},
  journal={Molecular cancer therapeutics},
  year={2012},
  volume={11 8},
  pages={
          1637-49
        }
}
SAR131675 is a potent and selective VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC(50) values of 20 and 45 nmol/L, respectively. SAR131675 dose dependently inhibited the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC(50) of about 20 nmol/L. SAR131675 was found to be highly selective for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. However, it… CONTINUE READING

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A Biological basis of therapeutic lymphangiogenesis

C Norrmen, T Tuomas, TV Petrova, Kari
  • Circulation
  • 2011
VIEW 3 EXCERPTS