VEGFR Tyrosine Kinase Inhibitor II

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit (IC₅₀ = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC₅₀ = 7.0 µM and 7.3 µM). Also displays antiangiogenic and antitumor properties. Does not inhibit the activities of CDK-1, c-Met, IGF-1R or PKA (IC₅₀ >10 µM).

A pyridinyl-anthranilamide compound that displays both antiangiogenic and antitumor properties. A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit (IC₅₀ = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC₅₀ = 7 µM and 7.3 µM). Further, inactive towards the inhibition of CDK-1, c-Met, IGF-1R and PKA (IC₅₀ >10 µM).

Cell permeable: yes

Primary Target
Kinase activities of KDR, Flt-1 and c-Kit

Product competes with ATP.

Reversible: yes

Target IC₅₀: 20 nM, 180 nM and 240 nM against kinase activities of KDR, Flt-1 and c-Kit, respectively

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Furet, P., et al. 2003. Bioorg. Med. Chem. Lett.13, 2967.

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

Toxicity: Standard Handling (A)