Table 1.

Inhibition of cell growth by lapatinib and neratinib

IC50 (nmol/L)a
CellLapatinibNeratinib
MCF10AHER2 WT480 ± 50<2
K753E>10,00032 ± 8
L768S1,050 ± 480<2
V773L960 ± 380<2
R647K650 ± 370<2
I655V520 ± 420<2
K676R385 ± 270<2
Q680R550 ± 190<2
BT47472 ± 24<2
HER2 WT109 ± 36<2
K753E1,240 ± 46040 ± 8
L768S286 ± 110<2
V773L218 ± 85<2
R647K86 ± 40<2
I655V120 ± 52<2
K676R64 ± 36<2
Q680R78 ± 5<2
MDA-MB-231HER2 WT3,620 ± 860410 ± 140
K753E>10,000889 ± 215
L768S4,890 ±1110590 ± 165
V773L4,980 ± 785780 ± 184
R647K3,578 ± 759472 ± 106
I655V3,496 ± 808508 ± 108
K676R3,730 ± 960537 ± 124
Q680R3,778 ± 845496 ± 98
MCF7>10,000>3,000
  • NOTE: Cells were incubated with certain drugs for six days, and cell viability was measured using CCK8 assay.

  • aMean IC50 (nmol/L) ± SD from three independent determinations.