VATALANIB DIHYDROCHLORIDE

Biochem/physiol Actions

Vatalanib (PTK787, ZK 222584, CGP 79787D, CGP 79787 succinate) is an orally active anilinophthalazine derivative that exerts its anti-angiogenic efficacy by targeting receptor tyrosine kinase (RTK) VEGFR (VEGFR1/2 IC50 = 54/39 nM; IC50 ~30 nM against 100 ng/mL VEGF-C-induced VEGFR3 autophosphorylation in MEVCs) and, to a less extent, PDGFRβ, c-kit, c-fms (IC50 = 364, 600, 567 nM, respectively) in an ATP-competitive manner with much reduced or no potency toward >90 other kinases. Typical dosing ranges: 0.1-10 µM in cultures, 5 nM-200 µM (zebrafish) and 30-100 mg/kg (mice & rats via po. or ip) in vivo.