VEGFR-2-IN-9

VEGFR-2-IN-9 (KDR-in-4) is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC₅₀ of 7 nM. IC50 & Target: IC50: 7 nM (KDR)^[1] In Vitro: KDR (kinase insert domain-containing receptor) is one of the human tyrosine kinases that has a high affinity for vascular endothelial growth factor (VEGF) and is believed to be a primary mediator of tumor-induced angiogenesis^[1]. In Vivo: KDR-in-4 may prove to be useful for the treatment of a variety of ocular neovascular diseases using a convenient oral dosing regimen. At doses of 100 mg/kg, KDR-in-4 results in a 98% reduction in lesion size in the rat choroidal neovascularization (CNV) model. 30 mg/kg doses of KDR-in-4 shows a 70% and 80% reduction in lesion size in the laser CNV and rat oxygen induced retinopathy (OIR) models, respectively^[2].