In this article, we expanded the targeted effect of (20S)G-Rh2, and systematically described its inhibition towards STAT3 and downstream VEGFs, suggesting the possibility that (20S)G-Rh2 interfered tumor micro-environment, providing new molecular basis and strategies for the further utilization of (20S)G-Rh2 in cancer therapy and research. This evidence concerns the gene STAT3 and neoplasm.