A selective antagonist of the activation of VEGFR-3 by VEGF-C (IC50 = 1 µM); does not inhibit ligand-induced autophosphorylation of VEGFR-2

MAZ51 – 10 mg

Brand:
Cayman
CAS:
163655-37-6
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

A selective antagonist of the activation of VEGFR-3 by VEGF-C (IC50 = 1 µM); does not inhibit ligand-induced autophosphorylation of VEGFR-2, EGFR, IGF-1R, or PDGFRβ; reduces proliferation and induces apoptosis in a variety of cancer cells in vitro and suppresses tumor growth in vivo

Formal name: 3-[[4-(dimethylamino)-1-naphthalenyl]methylene]-1,3-dihydro-2H-indol-2-one

Synonyms: 

Molecular weight: 314.4

CAS: 163655-37-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors

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