TAS 6417

TAS 6417 is a pan-EGFR inhibitor.¹ It inhibits wild-type EGFR (IC₅₀= 8 nM), as well as the EGFR point mutants EGFR^L858R, EGFR^L861Q, EGFR^T790M, EGFR^T790M/L858R (IC₅₀s = 1.9, 5.5, 4.1, and 2 nM, respectively) and the insertion or deletion mutants EGFR D770_N771insNPG, EGFR d746-750, and EGFR d746-770/T790M (IC₅₀s = 7.4, 1.4, and 1.1 nM, respectively). It is selective for these kinases over a panel of 20 additional kinases (IC₅₀s = 44-850 nM) but does inhibit TXK, BMX, HER4, Tec, and BTK (IC₅₀s = 1.1-22 nM). TAS 6417 inhibits the proliferation of LXF 2478L, H1975, HCC827, and PC-9 lung cancer cells (GI₅₀s = 86.5, 45.4, 1.92, and 2.96 nM, respectively). In vivo, TAS 6417 (50, 100, and 200 mg/kg) reduces tumor volume and increases survival in an H1975 EGFR D770-N771insSVD mouse xenograft model.

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1. Hasako, S., Terasaka, M., Abe, N., et al. TAS6417, a novel EGFR inhibitor targeting exon 20 insertion mutations. Mol. Cancer Ther. 17(8), 1648-1658 (2018).