Recently, carbon dots (CDs) have been actively studied and reported for their various properties. In particular, the specific characteristics of carbon dots have been considered as a possible technique for cancer diagnosis and therapy. This is also a cutting-edge technology that offers fresh ideas for treating various disorders. Though carbon dots are still in their infancy and have not yet shown their value to society, their discovery has already resulted in some noteworthy advancements. The application of CDs indicates conversion in natural imaging. Photography using CDs has demonstrated extraordinary appropriateness in bio-imaging, the discovery of novel drugs, the delivery of targeted genes, bio-sensing, photodynamic therapy, and diagnosis. This review seeks to provide a comprehensive understanding of CDs, including their benefits, characteristics, applications, and mode of action. In this overview, many CD design strategies will be highlighted. In addition, we will discuss numerous studies on cytotoxic testing to demonstrate the safety of CDs. The current study will address the production method, mechanism, ongoing research, and application of CDs in cancer diagnosis and therapy.