Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetVEGF receptor tyrosine kinase

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.

Cell permeable: yes

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Warning

Toxicity: Standard Handling (A)