| 货号 | 16168-25mg |
| 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.1 MAZ51 is an indolinone that selectively antagonizes the activation of VEGFR3 by VEGFC (IC50 = 1 µM) without blocking VEGFC-mediated stimulation of VEGFR2.2 It does not inhibit ligand-induced autophosphorylation of EGFR, IGF-1R, or PDGFRβ.3 By preventing VEGFR3 activation, MAZ51 interferes with an autocrine loop involving the induced expression of the ligand VEGFC as well as VEGFA.4 It reduces proliferation and induces apoptosis in a variety of cancer cells in vitro and suppresses tumor growth in vivo.3 MAZ51 is used to study the role of VEGFR3 in endothelial and cancer cell function and survival.5,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Manley, P.W.,Bold, G.,Brüggen, J., et al. Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis. Biochim.Biophys.Acta. 1697(1-2), 17-27 (2004). 2.Kirkin, V.,Mazitschek, R.,Krishnan, J., et al. Characterization of indolinones which preferentially inhibit VEGF-C- and VEGF-D-induced activation of VEGFR-3 rather than VEGFR-2. European Journal of Biochemistry 268(21), 5530-5540 (2001). 3.Kirkin, V.,Thiele, W.,Baumann, P., et al. MAZ51, an indolinone that inhibits endothelial cell and tumor cell growth in vitro, suppresses tumor growth in vivo. International Journal of Cancer 112(6), 986-993 (2004). 4.Matsuura, M.,Onimaru, M.,Yonemitsu, Y., et al. Autocrine loop between vascular endothelial growth factor (VEGF)-C and VEGF receptor-3 positively regulates tumor-associated lymphangiogenesis in oral squamoid cancer cells. American Journal of Pathology 175(4), 1709-1721 (2009). 5.Park, J.H.,Shin, Y.J.,Riew, T.R., et al. The Indolinone MAZ51 Induces Cell Rounding and G2/M Cell Cycle Arrest in Glioma Cells without the Inhibition of VEGFR-3 Phosphorylation: Involvement of the RhoA and Akt/GSK3ß Signaling Pathways. PLoS One 9(9), 1-9 (2014). 6.Breslin, J.W.,Yuan, S.Y. and Wu, M.H. VEGF-C alters barrier function of cultured lymphatic endothelial cells through a VEGFR-3-dependent mechanism. Lymphat.Res.Biol. 5(2), 105-113 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 314.4 |
| 分子式 | C21H18N2O |
| CAS号 | 163655-37-6 |
| 稳定性 | ≥ 2 years |
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