产品描述:
DZD9008 is an irreversible inhibitor of EGFR containing a lysine-to-arginine mutation at position 858 and T790M (EGFRL858R,T790M; IC50 = 1.1 nM).{68618} It is selective for EGFRL858R,T790M over Bruton's tyrosine kinase (BTK), wild-type EGFR, focal adhesion kinase (FAK), HER2, and HER4 (IC50s = 213, 226, 255, 392, and 704 nM, respectively) but also inhibits wild-type EGFR containing an exon 19 deletion, EGFRT790M containing an exon 19 deletion, EGFRL585R, EGFRG192A, and EGFRL861Q (IC50s = 1.3-12 nM). DZD9008 (25 and 50 mg/kg twice per day) reduces tumor volume in a patient-derived xenograft (PDX) mouse model of non-small cell lung cancer (NSCLC).