Vatalanib Dihydrochloride

Description

Vatalanib is an antagonist of the VEGF receptors, inhibiting the receptor tyrosine kinase activities of VEGFR1 (Flt1), VEGFR2 (KDR), and VEGFR3 (Flt4) with IC₅₀ values of 77, 37, and 190 nM, respectively. It less potently inhibits PDGF and c-Kit (IC₅₀ = 600 and 700 nM) and has no effect on a large panel of additional kinases. Vatalanib completely blocks retinal neovascularization in oxygen-induced ischemic retinopathy in mice, suggesting its use in diabetic retinopathy and other diseases featuring aberrant vascular development.

Chemical properties

White to Off-White Crystalline Powder

The Uses of Vatalanib Dihydrochloride

Vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor. Antineoplastic.

The Uses of Vatalanib Dihydrochloride

Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR, Flt-1 and c-Kit with IC50 of 37 nM, 77 nM and 730 nM, respectively.

What are the applications of Application

Vatalanib Dihydrochloride is a potent inhibitor of EGFR- and RET-dependent tumor cell proliferation and survival

References

1) Wood?et al. (2000),?PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration;? Cancer Res.,?60?2178 2) Lin?et al. (2002),?The vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584 inhibits growth and migration of multiple myeloma cells in bone marrow microenvironment;? Cancer Res.,?62?5019