With the beginning of the new millennium, a new and exciting era for cancer therapy has begun with theappearance of molecular targeted drugs. Imatinib is a clinically well-tolerated small molecule that exerts selective,dual inhibition of the transforming growth factor beta (TGFbeta) and platelet-derived growth factor (PDGF)pathways. Imatinib is also suggested as a chemopreventive for recurrent and metastatic malignancies. Aninteresting point to be clarified regarding the mechanism of imatinib is its interaction with c-Src. Fortunately,complexing of c-Src and imatinib has recently reported, which provides a basis for further study of the interactionsbetween the two molecules. In the present study, the author used the technique named molecular dicing to studythe interaction surface between the two molecules. Accordingly, the interaction surface in c-Scr and imatinibcould be identified.