EGFR-IN-182

EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer[1].

Product Specifications

Target

Akt; Apoptosis; Caspase; CDK; EGFR; ERK; HSP; PI3K

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; JAK/STAT Signaling; MAPK/ERK Pathway; Metabolic Enzyme/Protease; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer

Smiles

N1(CC2=CC=CC=C2)C3=NC(N/N=C/C4=NC(C=CC=C5)=C5N=C4)=NN=C3C6=C1C=CC=C6

Molecular Formula

C25H18N8

Molecular Weight

430.46

References & Citations

[1]Ezz-ElDien ES, et al. Design, synthesis, and antiproliferative efficacy of an innovative series of triazino[5,6-b]indole derivatives targeting EGFR, CD1, Hsp90, PI3K, and ERK/AKT as key molecular targets in cancer therapy. Eur J Med Chem. 2025 Oct 16;302 (Pt 1) :118263.