EGFR-IN-208 

EGFR-IN-208 is an allosteric mutant EGFR^L858R/T790M and EGFR^{L858R/T790M/C797S} inhibitor, with IC₅₀ values of 3.06 μM and 1.08 μM, respectively. EGFR-IN-208 binds to the allosteric site of EGFR and inhibits EGFR phosphorylation. EGFR-IN-208 induces apoptosis and exhibits antiproliferative effects in cancer cells. EGFR-IN-208 can be used in research related to non-small cell lung cancer^[1].

EGFR-IN-208 (Compound 2b) potently inhibits the proliferation of A549 (EGFR^WT), H3255 (EGFR^L858R), PC-9 (EGFR^Del19), H1975 (EGFR^L858R/T790M) and Ba/F3 (EGFR^{L858R/T790M/C797S}) cells, with IC₅₀ values ranging from 1.08 μM to 4.33 μM, and exhibits the strongest inhibitory activity against Ba/F3 cells^[1].
EGFR-IN-208 (0.1-3 μM) inhibits EGFR phosphorylation in a concentration-dependent manner in H1975 cells and Ba/F3-EGFR^{L858R/T790M/C797S} cells without altering the total EGFR protein level^[1].
EGFR-IN-208 (0.5-5 μM; 48 h) induces apoptosis in H1975 cells and Ba/F3-EGFR^{L858R/T790M/C797S} cells in a dose-dependent manner within 48 hours, with apoptosis rates ranging from 12.98% to 51.8% across the tested concentration range^[1].

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

519.61

C₃₂H₃₀FN₅O

3087298-90-3

CC1=CC(NC(C2=CC=C3C=CC(C4=CC=C(C=C4)N5CCNCC5)=NC3=C2O)C6=CC(F)=CC=C6)=NC=C1

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• [1]. Xu X, et al. Discovering potent EGFR inhibitors through the structural optimization of the Betti-base scaffold. Bioorg Med Chem Lett. Published online March 25, 2026.