Introduction: Tanacetum dolicophyllum (Kitam.) Kitam is recognized for its pharmacacological and ethnomedical significance. The compound derived from T. dolicophyllum demonstrated important antioxidant activity, indicating its advanced antioxidant potentials. Objectives: To examine the bioactive component isolated from T. dolicophyllum, specifically focuses on its antioxidant and anticancer characteristics. Methods: The compound isolation process commenced with column chromatography and thin layer chromatography techniques which was then characterized by FT-IR, 1H NMR, 13C NMR, and HRMS to elucidate its chemical structure and functional groups. Then their biological activity was evaluated which involves antioxidant and anticancer assays. Results: FT-IR, NMR, and HRMS studies of the compound showed the characteristics peaks of functional groups like alkanes, alkynes, ketones, peroxides and esters which show anticancer and antioxidant properties. The anti-cancer activity was investigated by the MTT assay whose IC50 value of the A549 cell line is 11 µM/ml. Conclusion: This research represents the characterization of the bioactive compound derived from T. dolicophyllum highlighting its antioxidant, anticancer, and pharmacologically active properties. These findings may pave the way for the creation of novel cancer therapeutics.