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 was found to be highly selective for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is the first highly specific VEGFR-3-TK inhibitor described to date, displaying significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.
LY2874455; ZM-306416; ZM323881; Tyrphostin A9; Orantinib; Brivanib; Foretinib; SU5402; Semaxanib; Lucitanib; Apatinib; SKLB610; Altiratinib; SGI-7079; AZD2932