Plant extracts and derived active principles have served as a major source for new pharmaceuticals for treatment of malignant tumors. Sambacaitá is a plant popularly utilized in the treatment of cancer and other diseases. The chemical studies of this plant extracts showed the presence of monoterpenes (especially cymene, thymol and β-terpinene) in a greater proportion in the essential oil and of a 2(5H)-furanone and α- pyrones in a dichloromethane extract obtained from this plant. In view of the popular utilization of this plant in cancer treatment, we decided to perform an evaluation of its cytotoxic and antitumor properties. The plant was collected, identified, and the hydroethanolic extract was prepared. In the pharmacological approach, the follow assays were done: toxicity against brine shrimp Artemia salina, in vitro test against human tumor cell lines and in vivo evaluation using sarcoma 180 in mice. The phytochemical screening showed the presence of flavonoids, tanins, saponins and sterols. In the Artemia salina essay Hyptis pectinata was considered atoxic. In the preliminary in vitro assay Hyptis pectinata showed moderate cytotoxicity: 62% of inhibition against HCT-8line cells, presented no hemolytic effect and in the evaluation of the cytotoxicity activities against peripheral blood mononuclear cells, showednon-toxicity. In the in vivotest, Hyptis pectinata inhibited the sarcoma 180 (70.5%). The histopathological analysis of the liver, kidneys and spleen of animals which was treated showed absence of lesions. Taken together these results suggest that Hyptis pectinata used by the population showed potential anti-tumor activity, at least at the presentin vitro and in vivo pharmacological models.