LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR). LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib. LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model[1].
