The aim of this study was to employ GC-MS to assess the biological potency and chemical composition of the aerial parts of Reichardia tingitana (L.) Roth. Using this technique, 16 components were interpreted from the extracted plant, accounting for 100% of total volatile compounds. Commonly, dodecane (5.43%), tetradecane (9.11%), ethyl palmitate (8.56%), methyl (E)-octadec-11-enoate (11.50%), 2-hydroxypropane-1,3-diyl(9E,9'E)-bis(octadec-9-enoate) (7.04%), lup-20(29)-en-3-ol (Lupeol) (10.81%), and olean-12-en-3-one (23.99%) are positioned as the major components. Fatty acids and their esters are the major categories (38.06%), steroids (34.8%) and hydrocarbons (24.11%). The DPPH antioxidant activity of the R. tingitana extracted components revealed that the shoot extract is the most powerful, with an IC50 value of 34.91 mg L-1 and a radical scavenging activity percentage of 60.35%. According to the current result, the 50% methanol crude shoot extract of R. tingitana showed greater potential anticancer activity with high cytotoxicity for two tumor cells HepG-2 and PC3 cells (IC50 = 90.55 and 79.27 µg mL-1, respectively), and non-cytotoxic activity for WI-38 normal cells (IC50 = >100 µg mL-1). R. tingitana is a promising plant with biological activity. Further work will involve isolation of pure compounds and determination of the bioactivity of individual compounds.