Uses
Naquotinib is an epidermal growth factor receptor (EGFR) inhibitor.
Biological Activity
Naquotinib (ASP8273) is an orally active, irreversible, mutant-selective epidermal growth factor receptor (EGFR) inhibitor with potential antitumor activity.
in vitro
ASP8273 is an irreversible TKI small molecule inhibitor that inhibits the kinase activity of EGFR mutants including T97M with limited activity against wild-type EGFR. In in vitro enzymatic activity and cellular assays, ASP8273 covalently bound to an EGFR mutant (L858R/T790M) through cysteine residues and long-term inhibited EGFR phosphorylation for 24 hours. In NSCLC cell lines with the above-mentioned EGFR mutations, ASP8273 has IC50 values in the range of 8-33 nM for EGFR mutants, more potent than WT EGFR (IC50 for WT EGFR is 230 nM).
