The disclosure provides a CD169 high affinity anti-tumor compound (TCC-Neu5A) and its preparation and application. The CD169 high affinity anti-tumor compound is a small molecule compound, which has specific and broad-spectrum tumor killing characteristics. TCC-Neu5Ac could targets tumor cells in vivo and metabolize onto a surface of the tumor cells to form CD169 ligands. These tumor cells are recognized and phagocytized by CD169-positive macrophages, which then release tumor-related antigens and present them to other immune cells, triggering an anti-tumor immune response. The CD169 high affinity anti-tumor compound provided by the disclosure is effective for a variety of tumors and has an inhibitory effect on tumor metastasis. In addition, the CD169 high affinity anti-tumor compound provided by the disclosure can not only be injected but also be orally administered. Cytotoxicity and animal toxicity of the CD169 high affinity anti-tumor compound are very low.