A new inhibitor of VEGF receptor tyrosine kinases, vegfrecine (1), was isolated from the culture broth of Streptomycessp. MK931-CF8. The molecular structure of 1was determined by NMR and MS analysis combined with synthesis. Compound 1showed potent inhibitory activity against vascular endothelial growth factor receptor (VEGFR) tyrosine kinases in in vitroenzyme assays, but platelet-derived growth factor receptors (PDGFRs), fibroblast growth factor receptor (FGFR), and epidermal growth factor receptor (EGFR) responded only weakly. Compound 1is a promising new selective VEGFR inhibitor for investigating new treatments of cancer and inflammatory diseases.