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

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

The Uses of Vatalanib Dihydrochloride

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

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