Drug intelligence / Profile preview

MAZ51

Development stage
Preclinical
Lead developer
Karlsruhe Institute of Technology
Modality
Small Molecules
Administration
Intraperitoneal, Subcutaneous (preclinical Animal Studies)
01

Overview

MAZ51 is a synthetic indolinone-based small molecule developed as a selective inhibitor of vascular endothelial growth factor receptor 3 (VEGFR-3/Flt-4) tyrosine kinase. It inhibits VEGFR-3 phosphorylation, thereby interfering with lymphangiogenesis and tumor cell proliferation. MAZ51 causes G2/M cell cycle arrest and cytoskeletal rearrangement in glioma and other tumor cell lines, acting through pathways such as Akt/GSK3β phosphorylation and RhoA activation. It exhibits antitumor activity in several preclinical models and inhibits proliferation of VEGFR-3-expressing and other tumor cells[1][2][3][4][5][6][8].

Other names
3-(4-Dimethylamino-naphthalen-1-ylmethylene)-1,3-dihydro-indol-2-oneVEGFR Tyrosine Kinase Inhibitor XVIVEGFR3 Kinase InhibitorVEGFR-3 Kinase InhibitorVEGFR 3 Kinase Inhibitor
02

Targets

VEGFR3 (Vascular endothelial growth factor receptor 3)

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