TAS6417 是一种高效的、具有口服活性的EGFR突变型抑制剂，可独特的结合到 EGFR 铰链区的 ATP 结合位点，其IC50值为 1.1-8.0 nM。

TAS6417 is an EGFR inhibitor and is an efficacious drug candidate for patients with NSCLC (IC50: ranging from 1.1-8.0 nM).

TAS6417 inhibits the growth of cells expressing exon 20 insertion mutations of the EGFR gene (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 (mean GI50: 1.92±0.21 nM to 7.12±0.60 nM) [1].

TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues. TAS6417 induces persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models [1].

1661854-97-2

C23H20N6O

396.44

DMSO:125 mg/mL (315.31 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years