<p><em>Chrysanthemum cinerariifolium</em> (<em>C. cinerariifolium</em>) is an empirically proven medicinal plant that has anticancer activities. This study aimed to profile metabolites, and cytotoxic activity of root, leaf, stem, and root extracts <em>C. cinerariifolium</em> on T47D cells and to determine the correlation of metabolite content with cytotoxic activity. The metabolite profile was carried out using UPLC-QToF-MS / MS, and cytotoxic activity was carried out using the MTT method. The results obtained in the form of a chromatogram were processed with the application <em>Masslynk</em> so that a metabolite profile data obtained. The data is then analyzed statistically using <em>Principal Component Analysis</em> (PCA). The results obtained on metabolite profiling showed that there were differences in metabolite profiles in the roots, stems, leaves, and chrysanthemums. The characteristic compounds in the flower section are <em>D - (-) - Morphine</em> and in the leaf part of <em>genistein </em> and <em>N - [(5-Chloro-1,2,3-thiadiazol-4-yl) methyl] -1- (2-isopropyl-4 -methyl-1,3-thiazol-5-yl) -N-methyl ethanolamine</em>. The major compounds in the roots, stems, and leaves are <em>Orphenadrine</em> with successive percentages of 9.11%, 10.16%, and 3.24%, and the major compounds in the flower section are <em>D - (-) - Morphine</em> with a percentage of 10, 86%. Furthermore, the results of the cytotoxic activity test showed differences in anticancer cytotoxic activity in the parts of the flower, leaf, stem, and root of <em>C. cinerariifolium</em>. Besides, there is a relationship between the metabolite content and anticancer cytotoxic activity of each part of <em>C. cinerariifolium</em>. The higher the level of orphenadrine compounds in the plant, the higher the potential for anticancer.</p><p> <strong>Keywords</strong>: <em>C. cinerariifolium</em>, UPLC-QToF-MS/MS, T47D cells.</p>