EGFR-IN-172 

EGFR-IN-172 is a EGFR inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC^[1].

EGFR-IN-172 (Compound 2b) shows high antiproliferative activity against A549 cells (EGFR^WT) (IC₅₀ = 5.31 μM), PC-9 cell (EGFR^T790M) (IC₅₀ = 0.55 μM), H1975 cells (EGFR^L858R/T790M) (IC₅₀ = 0.40 μM) and Ba/F3-EGFR^{L858R/T790M/C797S} cells (IC₅₀ = 2.36 μM)^[1].
EGFR-IN-172 (0.1-10 μM) inhibits the phosphorylation of EGFR (pEGFR) in H1975 and Ba/F3 triple-mutant cells in a concentration-dependent manner^[1].
EGFR-IN-172 (0.25-1 μM, 48 h) arrests the H1975 cells in the G0/G1 phase, but has no significant effect on the cell cycle of the Ba/F3 triple-mutant cells^[1].
EGFR-IN-172 (0.25-1 μM, 48 h) induces apoptosis in H1975 and Ba/F3 triple-mutant cells in a concentration-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

359.40

C₂₂H₁₈FN₃O

878416-74-1

OC1=C2N=CC=CC2=CC=C1C(C3=CC=CC(F)=C3)NC4=NC=CC(C)=C4

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• [1]. Xu X, et al. Design and synthesis of Betti base derivatives as EGFR inhibitors. Bioorg Chem. 2025 Sep;164:108872.