TQB3804 (EGFR-IN-7) is a selective, potent, 3rd generation EGFR C797S inhibitor with IC50 of 1.07 nM and 0.13 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively.
TQB3804 displays potent enzymatic activities for EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, and EGFRL858R/T790M with IC50 of 0.46, 0.13, 0.26, and 0.19 nM respectively, and has similar enzymatic activity for EGFRWT (IC50=1.07 nM) to Osimertinib.
TQB3804 shows expected anti-proliferative activity Ba/F3 (EGFRd746-750/T790M/C797S), NCI-H1975 (EGFRd746-750/T790M/C797S), PC9 (EGFRd746-750), and A431 (EGFRWT), with IC50 of 26.8, 163, 45, and 147 nM, respectively.
TQB3804 inhibits phosphorylation for EGFR in Ba/F3 (EGFRd746-750/T790M/C797S) cell line with IC50 of 18.5 nM.
TQB3804 significantly inhibits tumor growth in the triple mutant Ba/F3 (EGFRd746-750/T790M/C797S), NCI-H1975 (EGFRd746-750/T790M/C797S), and PC9 (EGFRd746-750/T790M/C797S) CDX models.