产品描述:
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.{26699} MAZ51 is an indolinone that selectively antagonizes the activation of VEGFR3 by VEGFC (IC50 = 1 µM) without blocking VEGFC-mediated stimulation of VEGFR2.{27479} It does not inhibit ligand-induced autophosphorylation of EGFR, IGF-1R, or PDGFRβ.{27480} By preventing VEGFR3 activation, MAZ51 interferes with an autocrine loop involving the induced expression of the ligand VEGFC as well as VEGFA.{27477} It reduces proliferation and induces apoptosis in a variety of cancer cells in vitro and suppresses tumor growth in vivo.{27480} MAZ51 is used to study the role of VEGFR3 in endothelial and cancer cell function and survival.{27478,27476}