EGFR-IN-200 

EGFR-IN-200 is an inhibitor targeting EGFR, TNF-α, and the IL-6/GP130 complex, which potently targets human EGFR (IC₅₀=0.03 μM), TNF-α (IC₅₀=3.1 μM), and the IL-6/GP130 complex (IC₅₀=1.6 μM). EGFR-IN-200 binds to the ATP pocket of EGFR, the trimer interface of TNF-α, and the cytokine-receptor interface of IL-6/GP130, induces G₂/M cell cycle arrest, apoptosis, and antiproliferative activity. EGFR-IN-200 exhibits high gastrointestinal absorbability, low BBB permeability, and complies with the Lipinski's rule. EGFR-IN-200 can be used for the research of lung cancer and breast adenocarcinoma^[1].

EGFR-IN-200 (compound 5h) potently inhibits the viability of A549 and MCF-7 cancer cells, with IC₅₀ values of 9.2 μM and 8.2 μM, respectively, and exhibits high selectivity toward malignant cells relative to non-tumorigenic cells^[1].
EGFR-IN-200 (0.01-100 μM; 1 h) potently inhibits EGFR tyrosine kinase activity with an IC₅₀ of 0.03 μM, and exhibits superior activity to Erlotinib (HY-50896)^[1].
EGFR-IN-200 binds directly to TNF-α and IL-6, with a K_d value of 2.3 μM for TNF-α binding and 1.8 μM for IL-6 binding^[1].
EGFR-IN-200 induces G2/M cell cycle arrest in A549 cells, blocks premitotic progression, and triggers apoptosis in A549 cells with a total apoptosis rate of 82.15%, with a preference for inducing early apoptosis^[1].

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

499.94

C₂₈H₂₂ClN₃O₄

3102899-89-5

ClC1=C(C2=C(C#N)C(OCC(NC3=C(OC)C=CC=C3)=O)=NC(C4=CC=C(OC)C=C4)=C2)C=CC=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Lotfy EM, et al. Microwave-assisted one-pot green synthesis, ADMET profiling, DFT, and molecular docking of novel 3-cyano-2-pyridone derivatives as dual EGFR and cytokine (TNF-α, IL-6) inhibitors. Eur J Med Chem. 2025;300:118165.  [Content Brief]