TY - JOUR AU - Qian Jing AU - Zhou Cai-Hong AU - Qian Zhen AU - Nan Fa-Jun AU - Ye Qi-Zhuang PY - 2016 TI - Development of a K562 cell-based assay for screening anticancer agents JF - Acta Pharmacologica Sinica; Vol 22, No 9 (September 2001): Acta Pharmacologica Sinica Y2 - 2016 KW - N2 - Aim: To develop a leukemia cell line K562-based assay for high-throughput screening. Methods: The screening was carried out on 96-well plates with monitoring cell proliferation by a combined 3-[4,5-dimethylthiazol-2-yl]-5-[3-carboxymethoxyphenyl]-2-[4-sulfophenyl]-2H-tetrazolium (MTS)/phenazine methosulfate (PMS) method. Conditions for evaluating effects on the proliferation of K562 cells by individual compounds on the 96-well plates were optimized. Results: A set of 800 small organic compounds was screened for anticancer activity by this cell-based assay, with consumption of each compound at 500 ng. Eleven compounds were identified with >80 % inhibitory activity at 5 mg/L, among which 9 compounds were confirmed by subsequent testing at multiple concentrations. The most potent compound showed an IC50 at 170 nmol/L, and there were total of 7 compounds showed IC50 less than 10 micromol/L. Conclusion: The high-throughput method using K562 cell line is fast, economical, effective, and practical in identifying inhibitors as potential therapeutic agents for cancer. UR - http://www.chinaphar.com/article/view/7603