Abstract: Pancreatic cancer is one of the most common malignancies of digestive tract. The targeted therapeutic drugs and specific diagnostic probes for pancreatic cancer include antibodies, affinity ligands, polypeptides, and small-molecule protein kinase inhibitors. The research on small-molecule protein kinase inhibitors is a hot topic of both preclinical research and clinical application in recent years. The advances in this area were briefly reviewed in this article. Data indicated that H-89, a kind of isoquinoline sulfonamide small molecule, might be one of the best small-molecule protein kinase inhibitors to treat pancreatic cancer, and if labeled with positron emitter, it might become a potential PET tracer for pancreatic cancer.