MAZ51
Cat. No.:YN440171
产品名称: | MAZ51 |
CAS No.: | 163655-37-6 |
Chemical Name: | 3-[[4-(dimethylamino)-1-naphthalenyl]methylene]-1,3-dihydro-2H-indol-2-one |
Synonyms: | |
分子量: | 314.38 |
分子式: | C₂₁H₁₈N₂O |
SMILES: | CN(C1=C2C=CC=CC2=C(C=C1)/C=C3C(NC4=C/3C=CC=C4)=O)C |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | MAZ51 是VEGFR-3酪氨酸激酶的选择性抑制剂。MAZ51 抑制 VEGF-C 诱导的 VEGFR-3 激活,而没有阻断 VEGF-C 介导的VEGFR2 刺激。MAZ51 对配体诱导的 EGFR,IGF-1R 和 PDGFRβ 的自磷酸化没有影响。MAZ51 阻止增殖并诱导多种肿瘤细胞凋亡。具有抗肿瘤活性。 |
IC50和靶点: | |
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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 angiogenesisBiochim. Biophys. Acta1697(1-2),17-27(2004)
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-2Eur. J. Biochem.268(21),5530-5540(2001)
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 vivoInt. J. Cancer112(6),986-993(2004)
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 cellsAm. J. Pathol.175(4),1709-1721(2009)
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 PathwaysPLoS One9(9),1-9(2014)
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 mechanismLymphat. Res. Biol.5(2),105-113(2007)