Combined with molecular docking model,quenching fluorescence,synchronous fluorescence,tridimensional fluorescence and UV-Vis absorption spectroscopy were applied to investigate the interactions of 4-methoxy-N-［4-(3-morpholin-4-yl-propoxy)-phenyl］-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide(1z) and human serum albumin(HSA) under simulative physiological conditions(pH 7.4) at the temperature of 298 K and 310 K,and the interaction mechanism was studied.The results showed that the quenching of 1z to HSA is probably a static process,and the conformation of HSA altered with the addition of 1z.The combination of theoretical research and experimental result provides a basis for studying the action mechanism of protein with drug,which further provides a certain experimental basis for study of small molecules of drugs in treatment of chronic myeloid leukemia.