General description

An orally bioavailable pyrrolopyrimidinylurea compound that simultaneously binds to both the adenine and the adjacent hydrophobic pocket of the inactive form of VEGFR2 with high-affinity (type-II inhibitor) and acts as a pseudo-irreversible inhibitor with prolonged action. Shown to potently inhibit the activities of VEGFR2, VEGFR1, Tie-2, PDGFRα, PDGFRβ and c-kit (IC₅₀ = 6.2, 15, 20, 35, 96 and 170 nM, respectively) with moderate to excellent selectivity over B-raf and Aurora-A (IC₅₀ = 0.9 and 1.05 µM) and FGFR1, HER2, EGFR, IR, PKCθ (>10 µM) among 18-kinases. Arrests VEGF-induced HUVECs proliferation (IC₅₀ = 4.4 µM) and suppresses DU145 carcinoma growth in a xenograft nude mouse model (6 mg/kg, b.i.d.).

Legal Information

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

Other Notes

Oguro, Y., et al. 2010. Bioorg. Med. Chem.18, 7150.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

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

Warning

Toxicity: Standard Handling (A)