Epidermal growth factor receptor(EGFR)is a potent target for the treatment of non-small cell lung cancer(NSCLC),however acquired resistance greatly limits the clinical efficacy of 1～3 generation inhibitors of EGFR.Compound A is a fourth generation EGFR inhibitor developed by BeiGene,Our structure-based medicinal chemistry effort yielded a Macrocyclic inhibitor of the EGFRde119/T790M/C797S and EGFRL858R/T790M/C797S mutants with an IC50 of 0.22 nmol/L and 0.20 nmol/L with high selectivity.
NETL
NSTL
万方数据
