Abnormal DNA methylation is one of the important mechanisms of tumorigenesis and development.It is the core of establishing and maintaining tissue-specific gene expression,and also the mechanism of regulating gene expression,which plays an important role in tumorigenesis.In parti-cular,the abnormal state of hypermethylation of tumor suppressor genes is of great significance in the occurrence,diagnosis,identification,prognosis and treatment of tumors.In addition,DNA methyla-tion and demethylation are reversible processes.5-Azacytidine can reduce the methylation level of hy-permethylated tumor suppressor genes by inhibiting DNA methyltransferase,so as to achieve the goal of tumor treatment.In leukemia,myelodysplastic syndrome,precursor bone marrow cell tumors and solid tumors,5-azacytidine inhibits cell proliferation and promotes cell differentiation through DNA dem-ethylation,which has therapeutic potential.However,its low bioavailability and long-term use may cause DNA damage and cytotoxicity.Therefore,it is necessary to find better administration methods and dose regulation strategies to verify and optimize its anti-tumor efficacy and promote clinical appli-cation.