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.
For research use only. We do not sell to patients.
- CAS No.: 3102899-89-5
- Formula: C28H22ClN3O4
- Molecular Weight:499.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
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 Kd 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.
Chemical Information
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CAS No. 3102899-89-5
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Molecular Weight 499.94
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Formula C28H22ClN3O4
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SMILES
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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)