EGFR-IN-173

EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT) . EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3) . EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research[1].

Product Specifications

UNSPSC

12352005

Target

Akt; Apoptosis; EGFR; ERK; p38 MAPK; STAT

Related Pathways

Apoptosis; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Smiles

CP(C)(C1=CC=CC=C1NC2=NC(NC3=CC(C4=CN(C)N=C4)=C(N(CCN(C)C)C)C=C3OC)=NC=C2Cl)=O

Molecular Formula

C28H36ClN8O2P

Molecular Weight

583.06

References & Citations

[1]Wang L, et al. Pan-EGFR inhibitor targeting EGFR 19del, L858R/T790M and C797S triple-mutations: Design, synthesis, and pharmacological evaluation. Bioorg Chem. 2025 Sep;164:108878.