EGFR-IN-206
EGFR-IN-206 is an orally active EGFR inhibitor. EGFR-IN-206 inhibits the phosphorylation of the key tumor growth protein EGFR, and suppresses the proliferation, migration and invasion of EGFR triple-mutant tumor cell lines. EGFR-IN-206 downregulates the expression of inflammation-related proteins iNOS, COX-2 and NF-κB (p65). EGFR-IN-206 promotes the secretion of NO. EGFR-IN-206 reduces the secretion of IL-6. EGFR-IN-206 induces apoptosis (apoptosis) of EGFR triple-mutant tumor cells. EGFR-IN-206 exerts antitumor activity in EGFR triple-mutant mice. EGFR-IN-206 is applicable to the research of non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C32H39N7O4S
- Molecular Weight:617.76
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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-206 (Compound 9f) potently inhibits the proliferation of three EGFR triple-mutant cancer cell lines, including Baf3-EGFRL858R/C797S/T790M (IC50 = 33.3 nM), Baf3-EGFRDel19/C797S/T790M (IC50 = 35.8 nM) and H1975-EGFRL858R/C797S/T790M (IC50 = 95.3 nM)[1].
EGFR-IN-206 (10-50 nM, 24 h) inhibits the migration and invasion of Baf3-EGFRL858R/C797S/T790M cells and H1975-EGFRL858R/C797S/T790M cells[1].
EGFR-IN-206 (50-500 nM) increases the proportion of dead cells in H1975-EGFRL858R/C797S/T790M 3D spheroids in a dose-dependent manner[1].
EGFR-IN-206 (10-1000 nM) reduces the mitochondrial membrane potential of Baf3-EGFRL858R/C797S/T790M and H1975-EGFRL858R/C797S/T790M cells in a dose-dependent manner, promotes cell apoptosis, and increases intracellular reactive oxygen species levels[1].
EGFR-IN-206 (10-1000 nM) dose-dependently inhibits the phosphorylation of EGFR in H1975-L858R/C797S/T790M cells without altering the expression level of total EGFR[1].
EGFR-IN-206 inhibits NO secretion in Raw264.7 and THP-1 cells stimulated by LPS (HY-D1056), with EC50 values of 101.4 nM and 144.7 nM, respectively[1].
EGFR-IN-206 (10-50 nM; 12 h) significantly reduces IL-6 secretion levels in LPS-stimulated Raw264.7 and THP-1 cells after 12 h of incubation[1].
EGFR-IN-206 (50-100 nM) inhibits the inflammation-enhanced colony-forming ability of H1975-L858R/C797S/T790M cells and reduces IL-6 secretion in the THP-1 co-culture model at a concentration of 50 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-stimulated Raw264.7, LPS-stimulated THP-1
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Concentration:10, 50 nM
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Incubation Time:12 h
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Result:Significantly reduced IL-6 secretion in both LPS-stimulated Raw264.7 and THP-1 cells compared to LPS-only controls.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice[1]
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Dosage:50 mg/kg
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Administration:p.o.; once daily; 7 days
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Result:Achieved a 67.3% tumor growth inhibition (TGI) rate.
Caused no obvious body weight changes, behavioral, or emotional abnormalities.
Significantly decreased expression levels of phosphorylated EGFR (p-EGFR) and COX-2 in tumor tissues.
Showed a negative correlation between p-EGFR levels and TGI.
Showed a negative correlation between COX-2 levels and TGI.
Showed a positive correlation between p-EGFR and COX-2 levels.
Chemical Information
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Molecular Weight 617.76
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Formula C32H39N7O4S
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SMILES
O=S(C1CC1)(NC2=CC=CC=C2NC3=C4C=C(OC)C(OC)=CC4=NC(NC5=CC=C(N6CCN(C)CCC6)C(C)=C5)=N3)=O
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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)