JIN-A02 showed high potency in EGFRex19del/T790M/C797S (IC50=4.7 nM, Ba/F3), EGFRL858R/T790M/C797S (IC50=12.8 nM, NCI-H1975 LTC). JIN-A02 strongly inhibited cellular activity of in trans model (IC50=89.7 nM, PDO) and in cis model (IC50=92.1 nM, PDC) of EGFRex19del/T790M/C797S....In the PDX mouse model (YHIM-1094, EGFRex19del/T790M/C797S), JIN-A02 delayed tumor growth at a dose of 30 mg/kg....JIN-A02 is highly potent EGFR-TKI for various EGFR targeted mutations including in cis and trans EGFRex19del/T790M/C797S and shows intracranial activity.