SU1498

SU1498 (CAS No.: 168835-82-3) is a small-molecule inhibitor classified as a selective antagonist of vascular endothelial growth factor receptor 2 (VEGFR2/Flk-1), a receptor tyrosine kinase central to angiogenic signaling. It exhibits inhibitory activity against VEGFR2 in the nanomolar range, with reported IC50 values around 700 nM, while showing minimal activity toward other kinases, supporting its utility as a relatively selective probe for VEGFR2-mediated pathways. SU1498 effectively suppresses VEGFR2-dependent signal transduction in both in vitro and in vivo systems, making it a valuable tool for investigating mechanisms underlying angiogenesis, tumor progression, and vascular biology. Mechanistically, it has been shown to modulate downstream signaling cascades, including effects on the MAPK/ERK pathway, where it can promote the accumulation of phosphorylated ERK under specific stimulatory conditions in endothelial cells, dependent on upstream components such as B-Raf and MEK. This compound is widely used in studies involving endothelial cell models, including human umbilical vein and aortic endothelial cells, as well as in animal models to dissect the role of VEGFR2 signaling in neural progenitor cell survival and neuroregeneration. Experimental concentrations and dosing regimens typically vary according to assay design and biological context, particularly in studies focused on pathway inhibition, target validation, and anti-angiogenic drug discovery.