Sodium new houttuyfonate (SNH) is volatile oil extracted from Houttuynia cordata Thunb. Its molecular formula is C14H27O5SNa, and molecular weight is 330.41. It is a new anti-inflammatory drug that has been used clinically over recent years. In this work, the binding interaction simulation study on SNH and epidermal growth factor receptor-tyrosine kinase (EGFR-TK) was conducted. SNH demonstrated a good binding ability to EGFR-TK and formed hydrogen-bonds with Cys773, Asp776, and Tyr777. This indicated that SNH might play an antitumor role as a potential inhibitor of EGFR-TK. In vitro, after treatment with various doses of SNH for 48 h, the viability of MCF-7 cells was 100.0, 98.23, 83.45, 76.24, 68.53, and 32.24, respectively, accompanied by a concentration increase in SNH. Moreover, cell viability of 250 μg/mL group decreased by more than 30%. Meanwhile, SNH significantly decreased cell cloning ability, and the quantities of clones were 456, 283, 137, and 152 in different groups (0 μg/mL, 100 μg/mL, 200 μg/mL, 250 μg/mL). In addition, SNH of different concentrations promoted the apoptosis of MCF-7 cells, which showed certain morphological characteristics of apoptotic cells including loss of cell adhesiveness, nuclear shrinkage, and appearance of apoptotic bodies. Furthermore, SNH effectively attenuated the migration of MCF-7 cells by decreasing the expressions of NF-kBp65 and vascular endothelial growth factor (VEGF). The increased number of apoptotic cells was also observed through hoechst33258 staining and Annexin V-PI staining, which corroborated with the decreased ratio of Bax and Bcl-2. Moreover, SNH induced the appearance of LC3 positive autophagosomes in MCF-7 cells. In vivo, SNH showed obvious antinematode activity, and LC50 was 40.46 μg/mL. Thus, SNH plays an antitumor role via regulating the apoptosis, autophagy, and migration of MCF-7 cells, and might act as a potential alternative drug in the treatment of breast cancer.