Objective: To investigate the anticancer activity of Helicteres hirsuta (H. hirsute) extract against a breast cancer cell line- MCF7. Methods: H. hirsute was extracted in absolute methanol. Further, the crude extract was further partitioned in n-hexane, chloroform and ethyl acetate. The total phenolic and flavonoid content were determined by using spectroscopic methods with gallic acid and quercetin standard compounds, respectively. Anticancer activities of H. hirsuta extract was elucidated by MTT, wound headling, and transwell invasion assays. Results: Total phenolic compounds in H. hirsute extracts reached 22.07 ± 2.54, 58.57 5.54 and 235.56 ± 7.54 mg GAE/g in each n hexan, chloroform, ethyl acetate fractions, respectively. Whereas the ethyl acetate fraction showed the greatest phenolic contents with 235.56 ± 7.54 mg GAE/g. Moreover, the flavonoid contents of H. hirsute extracts reached 5.76 ± 0.94, 9.25 ± 1.84 and 19.37 ± 2.57 mg quercetin equivalent/g in each n hexan, chloroform, ethyl acetate fractions, respectively, in which, the ethyl acetate fraction also showed the highest amounts of flavonoid contents. Further, the ethyl acetate of H. hirsute significantly decreased the viability of breast cancer MCF7 cells after 48 h treatment with IC50 value of 95 ± 2.54 \(\mu g/mL\) compared to control. In addition, the ethyl acetate extract of H. hirsute suppressed the invasion and migration of MCF7 cell lines in a dose-dependent manner at non-toxic concentrations. Conclusions: The ethyl acetate of H. hirsute suppressed the growth and motility of breast cancer MCF7 cells.