LYG-202 is a synthetic flavonoid with anticancer and anti-angiogenic activities. It inhibits proliferation of HepG2, MCF-7, HeLa, BGC-823, MDA-MB-435, and HCT116 cancer cells in vitro (IC50s = 4.74-27.70 μM) via induction of apoptosis and dissipation of the mitochondrial membrane potential. LYG-202 reduces tumor growth in S180 sarcoma cell-inoculated mice. It also inhibits VEGF-stimulated human umbilical vein endothelial cells (HUVEC) cell migration and tube formation in vitro and decreases capillary sprouting in isolated rat aortic rings and the chicken chorioallantoic membrane (CAM) model of angiogenesis.