A cell-permeable and reversible indolin-2-one class of receptor tyrosine kinase (RTK) inhibitor [IC₅₀ = 70 nM for VEGF-R2 (KDR/Flk-1), 920 nM for PDGF-Rβ, 4.92 µM for p60^c-src, and 13.3 µM for FGF-R1]. The inhibition is suggested to be competitive with respective to ATP. Also inhibits VEGF-induced (IC₅₀ = 110 nM) and PDGF-induced (IC₅₀ = 2.01 µM) cell proliferation in umbilical vein endothelial cells (HUVEC). Does not exhibit any inhibitory effect on EGF-R kinase activity (IC₅₀ >100 µM).

A membrane permeant and reversible indolin-2-one class of receptor tyrosine kinase (RTK) inhibitor [IC₅₀ = 70 nM for VEGF-R2 (KDR/Flk-1), 920 nM for PDGF-Rβ, 4.92 µM for p60^c-src, and 13.3 µM for FGF-R1]. The inhibition is suggested to be competitive with respect to ATP. Does not inhibit EGF-R kinase activity (IC₅₀ >100 µM).

Cell permeable: yes

Primary Target
VEGF-R2 (KDR/Flk-1)

Product competes with ATP.

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sun, L., et al. 2000. J. Med. Chem.43, 2655.

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

Toxicity: Standard Handling (A)