EGFR-IN-451

EGFR-IN-451 is an EGFR inhibitor with an IC₅₀ value of 0.02 nM. EGFR-IN-451 also inhibits mutant EGFR^L858R, EGFR^T790M, and EGFR^L858R/T790M with IC₅₀ values of 0.26-34 nM. EGFR-IN-451 inhibits AKT and ERK activation and inhibits proliferation of EGFR-mutant cancer cells. EGFR-IN-451 can be used for the research of EGFR-driven cancer^[1]. In Vitro:EGFR-IN-451 (Compound R14) (0.1-10000 nM) potently inhibits wild-type EGFR (IC₅₀ = 0.02 nM), EGFR^L858R (IC₅₀ = 0.26 nM), EGFR^T790M (IC₅₀ = 25 nM), and EGFR^L858R/T790M (IC₅₀ = 34 nM) in a cell-free caliper mobility shift assay^[1].
EGFR-IN-451 inhibits the viability of HCC827 cells (IC₅₀ = 2.47 μM) and H1975 cells (IC₅₀ = 18.07 μM) in an MTT assay^[1].
EGFR-IN-451 (0.01-10 μM; 1-12 h) inhibits phosphorylated EGFR in HCC827 cells at 0.01 μM and in H1975 cells at 0.1, 1, and 10 μM, with sustained reduction of phosphorylated EGFR in HCC827 cells over 12 h, and inhibits P-AKT, P-ERK expression^[1].