Insulin-like growth factors (IGFs) are homeostasis regulatory factors that participate in diverse physiological, synthetic and metabolic processes throughout the body and play key autocrine, paracrine and endocrine roles in promoting growth, involving the regulation of cell proliferation, differentiation and apoptosis in various tissues and organs. Numerousin vivo and in vitro experiments and clinical reports have found that the abnormal expression of IGF molecules plays a crucial role in the proliferation and invasion of various organ cancers, reproductive system cancers and other tumors. From a clinical perspective, IGF signaling axis can be recognized as potential biomarkers in diagnosis, prognosis, and therapy for cancer. Therefore, targeting the downstream molecular and signaling pathway changes caused by IGFs in different cancer tissues, combined with targeted molecular inhibitors for targeted drug use, may become a new way to treat cancer. Here, we summarize the changes of IGFs signaling in different tumor tissues, and include the small molecule inhibitors of IGFs axis. This review aims to provide guidance for future clinical treatment and research of cancer to a certain extent, and to provide some reference for the use of molecular targeted therapy as an adjunct to cancer drugs in the future.