Table 1.

Cellular potency of TAS6417

A. Inhibitory activity of TAS6417 against pEGFR in NIH/3T3 cell lines expressing human EGFR
IC50 value, nmol/L
EGFR statusMean ± SD
WT (+EGF)368 ± 181
A763_Y764insFQEA<4.48
V769_D770insASV78.2 ± 27.4
D770_N771insSVD23.4 ± 2.5
D770_N771insG45.7 ± 19.8
H773_V774insNPH66.7 ± 19.0
H773_V774insPH117 ± 31
Ex19del1.35 ± 0.17
Ex19del+T790M0.868 ± 0.152
B. Inhibitory activity of TAS6417 against cell proliferation in lung cancer cell lines and primary keratinocytes
GI50, nmol/L
TAS6417AfatinibErlotinib
Cell lineMean ± SDMean ± SDMean ± SD
LXF 2478L86.5 ± 28.571.7 ± 21.51040 ± 365
NCI-H1975 EGFR D770_N771insSVD45.4 ± 2.6221 ± 452340 ± 313
HCC8271.92 ± 0.211.61 ± 0.1310.0 ± 2.3
PC-92.96 ± 1.563.36 ± 1.7966.3 ± 22.6
NCI-H19757.12 ± 0.60182 ± 30>3,000
NCI-H23>3,0001710 ± 151>3,000
NCI-H460>3,000>3,000>3,000
NHEK-Neo729 ± 37333.2 ± 16.7557 ± 219