Tumors are significant diseases that pose a substantial threat to human health. Presently, there are diverse methods for diagnosing and treating tumors in clinical. However, real-time monitoring of the distribution of tumor cells within the body and precise tumor eradication remains a challenge. Recently, with the advancement of nanotechnology, the utilization of nanoparticle has enabled real-time monitoring of tumor cells migration and distribution within the body, as well as controlled and sustained drug release tailored to the specific tumor microenvironment (TME). This achievement has facilitated precise tumor eradication. Among various nanoparticle, graphene oxide (GO) boasts a substantial-specific surface area, which not only allows efficient drug loading but also effectively quenches the fluorescence signal of diagnostic molecules. When GO reaches the tumor tissue, the high concentration of glutathione (GSH) in the tumor environment reduces GO into reduced graphene oxide (rGO). This reduction triggers the release of fluorescent diagnostic molecules from its surface, leading to the restoration of their fluorescence signal and enabling timely tumor diagnosis. Furthermore, GO possesses strong near-infrared absorption and thermal conductivity properties. Hence, utilizing GO-based photothermal therapy, in addition to leverage its excellent photothermal conversion efficiency for direct tumor cells ablation, it achieves precise and sustained drug release based on the specific TME. Exploiting the distinctive biological properties of GO, this paper aims to provide a comprehensive overview of the latest research and related progress in the utilization of GO as a carrier for drugs and diagnostic agents in the realms of tumor diagnosis and precision treatment. First, we describe the biochemistry of GO and its application as a fluorescence quencher in tumor diagnosis. Second, capitalizing on GO's substantial surface area and environment-responsive attributes, we delve into the research progress of GO in tumor treatment. Finally, we summarize GO's biocompatibility as a drug carrier for tumor diagnosis and treatment while also discussing its future prospects.