TAS6417

1661854-97-2

C23H20N6O

DMSO : >= 125 mg/mL (315.31 mM)

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC₅₀ values ranging from 1.1-8.0 nM. IC50 & Target: 1.1-8.0 nM (EGFR)^[1]. In Vitro: TAS6417 inhibits the in vitro phosphorylation activity of EGFR and its mutants including an exon 20 insertion mutation, with IC₅₀ values ranging from 1.1+/-0.1 to 8.0+/-1.1 nM. TAS6417 suppresses the growth of cells expressing exon 20 insertion mutations of the EGFR gene, with a GI₅₀ value of 86.5+/-28.5 nM for LXF 2478L cells and 45.4+/-2.6 nM for NCI-H1975 EGFR D770_N771insSVD cells. TAS6417 also potently inhibits proliferation in other cell lines harboring activating mutations or acquired resistance mutations, with mean GI₅₀ values of 1.92+/-0.21 nM to 7.12+/-0.60 nM. In contrast, the effect of TAS6417 on cell proliferation in normal human epidermal keratinocytes (NHEK-Neo), of which WT EGFR is implicates in the growth and survival, is moderate^[1]. In Vivo: TAS6417 causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models. TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues. TAS6417 prolongs survival of animals bearing lung cancer^[1].