EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity.
EGFRT790M/L858R-IN-2 (compound 28f) (0.1, 1, 10 µM; 4 h) decreases the expression of p-EGFR, P-AKT, P-ERK1/2 in a dose-dependent manner in H1975, HCC827 cells[1].EGFRT790M/L858R-IN-2 (0.1, 1, 10 µM; 48 h) induces apoptosis and cell cycle arrest in the G1 phase in H1975, HCC827 cells[1].EGFRT790M/L858R-IN-2 (0.1, 1, 10 µM; 14 days) inhibits colony formation and cell migration in a dose-dependent manner[1].
EGFR T790M/L858R-IN-2 (5, 10, 20 mg/kg; i.p.; daily) inhibits tumor growth in a dose-dependent manner[1].Pharmacokinetic Parameters of EGFR T790M/L858R-IN-2 in Male Sprague-Dawley rats[1].
References:
[1]. Pei J, et al. Design, Synthesis, and Antitumor Activity of Potent and Selective EGFR L858R/T790M Inhibitors and Identification of a Combination Therapy to Overcome Acquired Resistance in Models of Non-small-cell Lung Cancer. J Med Chem. 2023 Apr 27;66(8):5719-5752.