Vatalanib hydrochloride (PTK787 hydrochloride) is an orally available and highly potent tyrosine kinase (VEGF) inhibitor that reduces the number and size of Aβ plaques in the cortex of 5xFAD mice, which may be useful in the study of Alzheimer's disease and cancer.

HUVEC:7.1 nM, c-Kit:730 nM, PDGFRβ:580 nM, Flk:270 nM

Vatalanib hydrochloride also inhibited Flk, c-Kit, and PDGFRβ with IC50s of 270 nM, 730 nM, and 580 nM, respectively.Vatalanib hydrochloride exerted its anti-proliferative effect in HUVECs by inhibiting VEGF-induced thymidine doping (IC50 of 7.1 nM) and dose-dependently inhibited VEGF-induced endothelial cell survival and migration over a similar dose range, with no significant cytotoxic or antiproliferative effects on cells not expressing VEGF receptors. [1]
Vatalanib hydrochloride significantly inhibited the growth of hepatocellular carcinoma cells and enhanced IFN/5-FU-induced apoptosis by elevating the level of Bax protein and reducing the expression of Bcl-xL and Bcl-2 proteins. [2]

Vatalanib hydrochloride administered orally once daily (25-100 mg/kg) dose-dependently inhibited angiogenic responses induced by VEGF and PDGF in growth factor implantation models and tumor cell-driven angiogenesis models. Vatalanib hydrochloride also effectively inhibited the growth and metastasis of several human cancers in nude mice at the same dose range, with no significant effect on circulating blood cells or bone marrow leukocytes. [1]