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Decsription: MAZ-51 is a novel, potent and selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRbeta. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
References:
1. KirkinV, et al. Characterization of indolinones which preferentially inhibitVEGF-C- and VEGF-D-induced activation of VEGFR-3 rather than VEGFR-2.Eur J Biochem. 2001 Nov; 268(21):5530-40.
2. KirkinV, et al. MAZ51, an indolinone that inhibits endothelial cell and tumorcell growth in vitro, suppresses tumor growth in vivo. Int J Cancer.2004 Dec 20; 112(6):986-93.
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