NS-062 (NS062) is a novel, specific targeted covalent inhibitor that shows high reactivity toward Cys797 of EGFR.
NS-062 showed higher target specificity for EGFR than the corresponding Michael acceptors in a wide concentration range (0.1-10 μM).
NS-062 showed strong antiproliferative activity (IC50=0.19 μM) against erlotinib-resistant H1975 cells (L858R T790M doublemutant EGFR).
NS-062 effectively inhibited EGFR (Y1068) autophosphorylation in H1975 cells at 0.5 uM, significantly suppressed tumor growth in a mouse xenograft model after oral administration.
