EGFR kinase inhibitor 1

EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

EGFR (WT):37 nM (IC50)

EGFRL858R/T790M:1.7 nM (IC50)

EGFRL858R/T790M/C797S:>300 nM (IC50)

EGFR kinase inhibitor 1 (compound 17i) (72 h) shows antiproliferative activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively[1]. EGFR kinase inhibitor 1 (0.05, 0.5, 5 µM; 48 h) induces apoptosis in a dose-dependent manner[1]. EGFR kinase inhibitor 1 (4, 20, 100 nM; 48 h) induces cell cycle arrest at G0/G1-phase[1]. EGFR kinase inhibitor 1 (0.5 μM; 0, 24, 48 h) inhibits the motility of the H1975 cells[1]. Cell Cytotoxicity Assay[1] Cell Line: A549, H1975 cells Concentration: Incubation Time: 72 h Result: Showed antiproliferation activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively. Apoptosis Analysis[1] Cell Line: H1975 cells Concentration: 0.05, 0.5, 5 µM Incubation Time: 48 h Result: Induced apoptosis in a dose-dependent manner. Apoptosis Analysis[1] Cell Line: H1975 cells Concentration: 4, 20, 100 nM Incubation Time: 48 h Result: Induced cell cycle arrest at G0/G1-phase with the percentage of G0/G1-phase cells increased from 42.93% to 60.52% at 4 nM, 70.39% at 20 nM and 80.03% at 100 nM.

[1]. Ding S, et al. Design, synthesis and biological evaluation of novel N-(3-amino-4-methoxyphenyl)acrylamide derivatives as selective EGFRL858R/T790M kinase inhibitors. Bioorg Chem. 2022 Jan;118:105471.