Therapeutic Discovery SAR 131675 , a Potent and Selective VEGFR-3 – TK Inhibitor with Antilymphangiogenic , Antitumoral , and Antimetastatic Activities

@inproceedings{Alam2012TherapeuticDS,
  title={Therapeutic Discovery SAR 131675 , a Potent and Selective VEGFR-3 – TK Inhibitor with Antilymphangiogenic , Antitumoral , and Antimetastatic Activities},
  author={Antoine Alam and Isabelle Blanc and eve Gueguen-Dorbes and Olivier Duclos and Jacques Bonnin and Pauline Barron and M. Laplace and Gaelle Morin and Florence Gaujarengues and Paul Schaeffer and Pierre Savi and Françoise Bono},
  year={2012}
}
SAR131675 is a potent and selective VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC50 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 IC50 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 was… CONTINUE READING

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