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In spite of advancements in cancer treatments, there is still a need for effective drugs against metastatic stages of breast cancer. Rheum emodi, a well known medicinal plant is not however extensively studied for its specific anticancer and anti-metastatic potentials. The present study evaluates the hot (CHR) and cold (CCR) chloroform extracts of R. emodi for its antioxidant properties through DPPH and reducing power assay, cytotoxicity in MDA-MB-231 and WRL-68 cells, and apoptosis inductivity in MDA-MB-231 and MCF-7 cells. Further, the anti-metastatic potential of CHR was also analysed by cell migration inhibition in MDA-MB-231 cells which is reported for the first time in this study. Both CHR and CCR exhibited efficient antioxidant properties, and significant cytotoxicity and apoptosis induction abilities. CHR had an exceptional ability to inhibit the migration of MDA-MB-231 cells. The extracts were then characterized semi-quantitatively and quantitatively to reveal its phytochemicals subsequent to HPLC analysis. Both CHR and CCR have demonstrated affirmative anticancer abilities with CHR also possessing capability to inhibit metastasis. Thus chloroform extracts of R. emodi could be considered in designing effective anticancer drugs especially against metastatic stages of breast cancer.