Recently, the use of porous nanomaterials with large mesopores, tunable porosity, and high surface area has drawn particular interest in the treatment and imaging of cancer. Adding additional pores to nanostructures alters therapeutic agent loading capacity and controlled release. It enhances optoelectronic and optical features suitable for tumor treatment. For many years, the leading cause of disease-related death has been cancer, which seriously threatens human health. Nanoscale-metal-organic frameworks are thought to have potential applications in the treatment and biomedical imaging of various tumors due to the rapid advancement of nanomedicine. Since their high surface area and porosity, ability to be customized in size, numerous physicochemical properties, ease of surface functionalization, and simplicity in synthesis, metal-organic frameworks (MOFs), an emerging porous organic-inorganic hybrid material, have gained popularity in recent years. These characteristics make them ideal carriers for cancer theragnostic applications. Although significant research has been done for the potential use of nanoscale MOFs (NMOFs) in cancer diagnostic and therapeutics, more information regarding the stability, in-vivo clearance, toxicology, and pharmacokinetics is still needed to enhance the use of NMOFs in cancer diagnostic and therapeutic. Different techniques using NMOFs are systematically summarized, including chemotherapy, photodynamic therapy (PDT), photothermal therapy (PTT), chemodynamical therapy (CDT), radiotherapy (RT), and the combined therapy methods. Finally, a brief conclusion and outlook for biomedical applications of this special field is provided