EGFR-IN-197 

EGFR-IN-197 is an EGFR inhibitor with IC₅₀ values of 19.5 nM and 12.0 nM against EGFR^L858R/T790M and EGFR^{L858R/T790M/C797S}, respectively. EGFR-IN-197 arrests the cell cycle of NCI-H1975 cells at the G2/M phase, while inhibiting their proliferation, colony formation and migration; it also inhibits mitochondrial translocation and upregulates mitochondrial H₂S levels. EGFR-IN-197 disrupts anti-apoptotic signaling pathways by regulating apoptosis-related proteins; it induces DNA damage and activates pro-apoptotic pathways to trigger apoptosis. EGFR-IN-197 can be used in studies related to non-small cell lung cancer (NSCLC)^[1].

EGFR-IN-197 (compound 6e) (72 h) potently inhibits proliferation of NCI-H1975, HCC827, and A431 cells with IC₅₀ values of 0.0473 μM, 0.0185 μM, and 0.0226 μM, respectively^[1].
EGFR-IN-197 potently inhibits EGFR^L858R/T790M and EGFR^{L858R/T790M/C797S} mutant kinases with IC₅₀ values of 19.5 nM and 12.0 nM, respectively^[1].
EGFR-IN-197 (0.05-0.5 μM; 14 d) concentration-dependently inhibits colony formation of NCI-H1975 cells^[1].
EGFR-IN-197 (0.05-0.5 μM; 12 h, 24 h) concentration-dependently inhibits migration of NCI-H1975 cells^[1].
EGFR-IN-197 (0.05-0.5 μM, 24 h) disrupts mitochondrial translocation of EGFR in NCI-H1975 cells^[1].
EGFR-IN-197 (0.05-0.5 μM, 24 h) concentration-dependently upregulates mitochondrial H₂S levels in NCI-H1975 cells^[1].
EGFR-IN-197 (0.005-0.5 μM; 24 h) concentration-dependently inhibits phosphorylation of EGFR and ERK1/2 in NCI-H1975 cells, and significantly inhibits AKT phosphorylation at 0.5 μM^[1].
EGFR-IN-197 (0.005-0.5 μM; 24 h) concentration-dependently modulates apoptosis-related proteins in NCI-H1975 cells, increasing Cleaved PARP and Cleaved caspase-3 and decreasing Bcl-xL^[1].
EGFR-IN-197 (0.1-1 μM; 24 h) concentration-dependently induces apoptosis in NCI-H1975 cells, with strong induction of late apoptosis at 0.5 μM and above^[1].
EGFR-IN-197 (0.05-0.5 μM; 24 h) concentration-dependently arrests NCI-H1975 cells at the G2/M phase, with 62.29% of cells in G2/M phase at 0.5 μM^[1].
EGFR-IN-197 (0.05-0.5 μM; 72 h) induces DNA damage in NCI-H1975 cells in a concentration-dependent manner, with significant damage observed at 0.1 μM and above^[1].

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

512.40

C₂₃H₂₆BrN₇O₂

3060883-16-8

CN(CC1)CCN1C(C=C2)=CC=C2NC3=NC=C(Br)C(NC4=CC=CC=C4C(NOC)=O)=N3

Room temperature in continental US; may vary elsewhere.

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

• [1]. Yang T, et al. Synthesis and mechanistic investigation of N-Alkoxybenzamide derivatives as EGFR inhibitors. Bioorg Chem. 2026;170:109530.  [Content Brief]