676492

VEGFR3 Kinase Inhibitor, MAZ51

The VEGFR3 Kinase Inhibitor, MAZ51, also referenced under CAS 163655-37-6, controls the biological activity of VEGFR3 Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): VEGFR3 Kinase Inhibitor, MAZ51, MAZ51, 3-(4-Dimethylamino-naphthalen-1-ylmethylene)-1,3-dihydro-indol-2-one, Vascular Endothelial Growth Factor Receptor 3 Kinase Inhibitor, VEGFR Tyrosine Kinase Inhibitor XVI, VEGFR3 Kinase Inhibitor I
• Empirical Formula (Hill Notation): C₂₁H₁₈N₂O
• CAS Number: 163655-37-6
• Molecular Weight: 314.38
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: red
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C21H18N2O/c1-23(2)20-12-11-14(15-7-3-4-9-17(15)20)13-18-16-8-5-6-10-19(16)22-21(18)24/h3-13H,1-2H3,(H,22,24)
• InChI key: VFCXONOPGCDDBQ-UHFFFAOYSA-N

Description

General description

A cell-permeable 3-substituted indolin-2-one compound that acts as a reversible and ATP-competitive VEGF receptor tyrosine kinase inhibitor. At low concentration (≤5 µM), it specifically blocks VEGF-C- (Cat. No. 676476) and VEGF-D- (Cat. No. 676471) induced phosphorylation of VEGFR-3, but not VEGFR-2, in PAE cells. It partially blocks VEGFR-2 phosphorylation only at higher concentrations (50 µM). This differential blocker may be useful for inhibiting lymphangiogenesis-dependent pathological process such as tumor metastasis. Not available for sale in Germany.

A cell-permeable, 3-substituted, indolin-2-one compound that acts as a reversible and ATP-competitive inhibitor of VEGF receptor tyrosine kinase. At low concentrations (5 µM), reported to specifically block VEGF-C and VEGF-D-induced phosphorylation of VEGFR-3, but not VEGFR-2, in PAE cells. Reported to partially block VEGFR-2 phosphorylation only at higher concentrations (50 µM). This differential inhibition may be useful for controlling lymphangiogenesis-dependent tumor metastasis and could, therefore, be of clinical significance for cancer therapy studies.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
VEGF receptor tyrosine kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: At low concentration (≤5 µM), it specifically blocks VEGF-C- and VEGF-D-induced phosphorylation of VEGFR-3, but not VEGFR-2, in PAE cells.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Kirkin, V., et al. 2001. Eur. J. Biochem.268, 5530

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3