Development of a K562 cell-based assay for screening anticancer agents

J. Qian, C. H. Zhou, Z. Qian, F. J. Nan, Q. Z. Ye

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


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-tetra zolium (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 μmol/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.

Original languageEnglish (US)
Pages (from-to)821-826
Number of pages6
JournalActa Pharmacologica Sinica
Issue number9
StatePublished - Sep 27 2001
Externally publishedYes


  • Antineoplastic agents
  • Antitumor drug screening assays
  • Cell culture
  • Drug screening
  • K562 cells

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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