Purpose: Herbal plants contain a great diversity of bioactive compounds with multiple targets and mechanisms of action for treating different types of cancers. So, the aim of this study to investigate antimicrobial, antitumor potential and chemical composition of the aerial parts of Aizoon canariense. Methods: Chemical profiling of methanol extract was determined by LC-ESI-TOF/MS technique. Isolation chemical constituents of ethyl acetate extract was carried out by chromatographic methods, identification and structure elucidation of these compounds was proven by spectroscopic methods. In-vitro antimicrobial activity was determined by diffusion agar technique according to CLSI, while cytotoxic effects were evaluated by the MTT assay method. Results: Sixty-one compounds included stilbene derivative, phenolic acids, flavonoids, and alkaloids were identified from methanol extract, in addition to six compounds were isolated and identified from ethyl acetate extract named cholic acid, syringetin, gossypetin, okanin-4'-glucosides, myrictrin, and datiscin. In vitro pharmacological studies showed the potency of ethyl acetate extract as antimicrobial agent against all tested gram-negative bacteria, and as antitumor agent against all tested carcinoma cell lines (hepatic, colon, and prostate) with safety influence on normal cell line. Conclusion: the results of this study and literature promote the efficiency of Aizoon canariense as potent antimicrobial and antitumor agent.