Abstract: Background and purpose: Fibroblast growth factor (FGF) family members can regulate cell proliferation, migration and differentiation and play an important role in tumorigenesis and metastasis. FGF receptor (FGFR) inhibitors have anti-tumor activity. This study investigated the effects of FGFR inhibitor BGJ398 on proliferation, migration, apoptosis and drug resistance of leukemia cell line K562/ADM. Methods: K562/ADM cells were divided into blank control group, negative control group and experimental group. The inhibition of K56/ADM cell proliferation was detected by cell counting kit-8 (CCK-8) assay, and the effect of BGJ398 on the migration ability of leukemia cells was detected by transwell assay. The apoptotic rate of each cell line was measured by flow cytometry, the sensitivity of K562/ADM cells to cytarabine (Ara-c) and daunorubicin (DNR) was detected by CCK-8 assay, and the effect of BGJ398 on MDR1 resistance gene was determined by Western blot. Results: The proliferation of K562/ADM cells was significantly inhibited by FGFR inhibitor BGJ398 in a concentration-dependent manner. BGJ398 inhibited K562/ADM cells at concentrations of 5, 10 and 15 μmol/L, respectively. Compared with the negative control group (57.67±14.57) and the blank control group (43.00±4.00), the number of transplanted cells in the experimental group was (11.00±3.00). The apoptotic rate in the experimental group was (81.49±5.38)%, compared with the control group (10.09±1.36)% and the negative control group (7.64±1.32)% (P<0.001). FGFR inhibitors significantly decreased the half maximal inhibitory concentration (IC ₅₀ ) of Ara-c and DNR to K562/ADM cells. Western blot showed that BGJ398 could significantly reduce the protein expression of MDR1 gene and reverse the drug resistance of leukemia cells. Conclusion: FGFR inhibitor BGJ398 can effectively inhibit the proliferation and migration of drug-resistant leukemia cell line K562/ADM, promote apoptosis and reverse drug resistance. FGFR may become a new target for the treatment of leukemia.

Key words: Fibroblast growth factor receptor inhibitor, K562/ADM cells, Leukemia