VEGFR Tyrosine Kinase Inhibitor IV - CAS 475108-18-0 - Calbiochem

A cell-permeable quinoline-urea compound that potently inhibits the kinase activity of VEGFR (IC₅₀ = 30, 6.5, and 15 nM for VEGFR-1,-2, and -3, respectively), EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2 (IC₅₀ = 24, 40, 49, 78, and 78 nM, respectively). It exhibits little or no activity towards a panel of 15 other tyrosine kinases, including FGFR, IR, and IGFR, in cell-free kinase assays, while showing more than 7-fold higher potency in inhibiting ligand-induced phosphorylation of VEGFR-1/2/3 vs. c-Kit, PDGFR-β, Flt3, FGFR1, and c-Met in cell-based assays. Shown to be orally available and suppress tumor angiogenesis and growth in rats in vivo.

A cell-permeable quinoline-urea compound that potently inhibits the kinase activity of VEGFR (IC₅₀ = 30, 6.5, and 15 nM for VEGFR-1,-2,and -3, respectively), EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2 (IC₅₀ = 24, 40, 49, 78, and 78 nM, respectively). It exhibits little or no activity towards a panel of 15 other tyrosine kinases, including FGFR, IR, and IGFR, in cell-free kinase assays, while showing more than 7-fold higher potency in inhibiting ligand-induced phosphorylation of VEGFR-1/2/3 vs. c-Kit, PDGFR-β, Flt3, FGFR1, and c-Met in cell-based assays. Shown to be orally available and suppress tumor angiogenesis and growth in rats in vivo.

Cell permeable: yes

Primary Target
VEGFR

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 30, 6.5, and 15 nM for VEGFR-1,-2, and -3, respectively; 24, 40, 49, 78, and 78 nM for EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2, respectively

Packaged under inert gas

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

Nakamura, K., et al. 2006. Cancer Res.66, 9134.

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

Toxicity: Standard Handling (A)