TAS6417,CAS#1661854-97-2
CAS No. 1661854-97-2 Cat. No. BCP30474
Name TAS6417
Synonyms TAS-6417;TAS 6417;
SMILES CC1=CC(CN2C1=C(C3=C2N=CN=C3N)C4=CC5=CC=CC=C5N=C4)NC(=O)C=C
Chemical Name
Formula C23H20N6O M. Wt 396.45
Purity 98% Storage Store at 4-8°C
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.