Croton caudatus Geisel is a traditional anticancer medicinal herb of the people of Mizoram, India. In the present study, the in vivo and in vitro anticancer potentials, antioxidant and analgesic properties of C. caudatus leaf extracts were evaluated. Phytochemical constituents of its methanol and aqueous extracts were also analyzed. Methanol (CC-Meth) and aqueous (CC-Aq) extracts exhibited potent anticancer activity in vivo (%ILS ̴ 92.5%) while in vitro cytotoxic activity was noted only with the aqueous extract. CC-Aq extract exhibited an IC50 value 28.36 µg/ml in vitro. The two extracts also significantly reduce acetic acid and formalin-induced pains in mice. The analgesic activity in both the first and second phases of formalin-induced pain test suggested that the extracts have both analgesic and anti-inflammatory properties. The aqueous extract showed significant DPPH and nitric oxide radical scavenging potentials. Results of preliminary phytochemical screening of aqueous extract of C. caudatus revealed the presence of alkaloids in larger amount and flavonoids, saponins, tannins and cardiac glycosides in lesser amount. The phytochemical constituents and antioxidant properties of the plant extract may be an important contributory factors involved in the anticancer and analgesic activities of aqueous extract of C. caudatus leaf.