TAS6417

Description	TAS6417 is a novel potent, selective inhibitor of EGFR exon 20 insertion mutations with IC50 of 1.1-8.0 nM, >100-fold selectivity over WT EGFR; fits into the ATP-binding site of the EGFR hinge region; inhibits EGFR phosphorylation and downstream molecules in NSCLC cell lines expressing EGFR exon 20 insertions (IC50=20-100 nM), resulting in caspase activation; inhibits the proliferation of Ba/F3 cells driven by various EGFR exon 20 insertion mutations with IC50 of 5.05-150 nM; causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models.
Pathways	Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway
Targets	EGFR

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