For the past few decades, cancer stem cells (CSCs) have elicited substantial research interest as important targets for consideration during cancer therapy. CSCs are notoriously drug resistant and are well known for their ability to undergo self-renewal and differentiation into more mature cancer cells, as well as for their tumour-initiating ability from a relatively small number of cells. However, to date, there has been a notable dearth of investigations regarding the exact role and functions of isolated populations of CSCs. In addition, the prevalence of CSCs in malignancy is still a matter of some debate and controversy. In this research, the aim was to identify specific CSC markers and to isolate the CSC subpopulations from colon cancers for study into ways of rendering them more susceptible to chemotherapy. Further, as there has been a limited number of studies focusing on identifying those drugs that can target the CSC enriched populations as therapeutic agents, a focus of this study was to examine and evaluate specific CSC surface markers for their identification and use. Specifically, the aims also included to examine the colorectal CSCs and identify drugs targeting purified CSCs in culture as well as in pre-clinical CRC models as a means of eliminating this type of cancer cell.