Table 1.

Antiproliferative activity of TAS0728 or afatinib for HER2-addicted cancer cell lines or EGFR-addicted cell lines

GI50b (nmol/L)
Cell linePrimary site of originGenetic alterationaTAS0728 (mean ± SD)Afatinib (mean ± SD)
SK-BR-3BreastHER2 Amplified5.0 ± 2.67.5 ± 1.4
AU565BreastHER2 Amplified5.1 ± 0.54.6 ± 0.8
BT-474BreastHER2 Amplified3.6 ± 0.53.0 ± 0.3
KPL-4BreastHER2 Amplified, PIK3CA mutated31 ± 7100 ± 29
NCI-N87GastricHER2 Amplified1.6 ± 0.31.0 ± 0.2
Calu-3LungHER2 Amplified6.9 ± 4.61.7 ± 1.2
A-431EpidermisEGFR Amplified450 ± 22014 ± 3
NHEK-Neo pooledKeratinocyte620 ± 31015 ± 10
  • aGenetic information was obtained from published articles.

  • bGI50: drug concentration causing 50% growth inhibition relative to the untreated control.