The VEGF receptors (VEGFRs) mediate signaling leading to angiogenesis, with VEGFR3 (FLT4), activated by VEGF isoforms VEGFC and VEGFD, primarily expressed on lymphatic endothelial cells and directing lymphangiogenesis. MAZ51 is an indolinone that selectively antagonizes the activation of VEGFR3 by VEGFC (IC50 = 1 μM) without blocking VEGFC-mediated stimulation of VEGFR2. It does not inhibit ligand-induced autophosphorylation of EGFR, IGF-1R, or PDGFRβ. By preventing VEGFR3 activation, MAZ51 interferes with an autocrine loop involving the induced expression of the ligand VEGFC as well as VEGFA. It reduces proliferation and induces apoptosis in a variety of cancer cells in vitro and suppresses tumor growth in vivo. MAZ51 is used to study the role of VEGFR3 in endothelial and cancer cell function and survival.
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MAZ51 is an indolinone compound that selectively antagonizes the activation of VEGFR-3 by VEGF-C without blocking VEGF-C mediated stumulation of VEGFR-2. This reduces proliferation and induces apoptosis in various cancer cells and suppresses tumor growth.
