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^[1].

EGFR-IN-206 (Compound 9f) potently inhibits the proliferation of three EGFR triple-mutant cancer cell lines, including Baf3-EGFR^{L858R/C797S/T790M} (IC₅₀ = 33.3 nM), Baf3-EGFR^{Del19/C797S/T790M} (IC₅₀ = 35.8 nM) and H1975-EGFR^{L858R/C797S/T790M} (IC₅₀ = 95.3 nM)^[1].
EGFR-IN-206 (10-50 nM, 24 h) inhibits the migration and invasion of Baf3-EGFR^{L858R/C797S/T790M} cells and H1975-EGFR^{L858R/C797S/T790M} cells^[1].
EGFR-IN-206 (50-500 nM) increases the proportion of dead cells in H1975-EGFR^{L858R/C797S/T790M} 3D spheroids in a dose-dependent manner^[1].
EGFR-IN-206 (10-1000 nM) reduces the mitochondrial membrane potential of Baf3-EGFR^{L858R/C797S/T790M} and H1975-EGFR^{L858R/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.

EGFR-IN-206 (50 mg/kg; p.o.; once daily; for 7 consecutive days) achieves a 67.3% tumor growth inhibition rate in nude mice bearing EGFR^{L858R/T790M/C797S} triple-mutant H1975 tumors, while reducing the intratumoral expression levels of p-EGFR and COX-2^[1].

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

617.76

C₃₂H₃₉N₇O₄S

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

• [1]. Tan Z, et al. Synthesis and evaluation of methoxyquinazoline sulfonamide derivatives as bifunctional molecular targeting tumor related inflammation and anti-EGFR triple-mutation. Bioorg Chem. 2026;173:109624.  [Content Brief]