EGFR-IN-185 

EGFR-IN-185 is a EGFR inhibitor. EGFR-IN-185 exhibits potent activity against non-small cell lung cancer (NSCLC) cells harboring EGFR mutations. EGFR-IN-185 inhibits colony formation and migration, induces G0/G1 arrest, and promots apoptosis, which are associated with the suppression of EGFR and AKT phosphorylation. EGFR-IN-185 can be used for the research of  NSCLC^[1].

EGFR-IN-185 (compound 33) (48 h) exhibits antiproliferation activity against NSCLC cells, with IC₅₀s of 3.1 (HCC827), 5.2 (H1975), 2.7 (H1975^TM), and 10.2 μM (A549)^[1].
EGFR-IN-185 (1-9 μM; 48 h) arrests the cell cycle progression of H1975^TM cells at the G0/G1 phase in a concentration-dependent manner^[1].
EGFR-IN-185 (0-10 μM; 0-24 h) inhibits H1975^TM cell migration in a concentration-dependent manner^[1].
EGFR-IN-185 shows negligible inhibitory activity against EGFR^WT, EGFR^19del, EGFR^L858R/T790M and EGFR^{L858R/T790M/C797S}, with IC₅₀ values of approximately 100, 20, 4, and 44 μM, respectively, suggesting that it does not function as an allosteric EGFR tyrosine kinase inhibitor^[1].
EGFR-IN-185 (2-10 μM, 20 h) exhibits strong antiproliferative effects on H1975^TM cells and suppresses the EGFR signaling pathway, as evidenced by the reduction of EGFR and AKT phosphorylation^[1].
EGFR-IN-185 (0-9 μM, 10 days) inhibits colony formation of H1975™ cells in a concentration-dependent manner^[1].
EGFR-IN-185 (2-8 μM, 32 h) inhibits H1975^TM cell growth through inducing cell apoptosis in a concentration-dependent manner^[1].

481.56

C₃₀H₂₈FN₃O₂

O=C1C2=CC(OCC3=CC=C(C4=CC=CC=C4)C=C3)=CC=C2NC5=C(C=C(F)C=C5)N1CCN(C)C

Room temperature in continental US; may vary elsewhere.

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

• [1]. Jin C, et al. Design, synthesis and structure-activity relationship analysis of dibenzodiazepinone derivatives against Osimertinib resistant NSCLC. RSC Med Chem. Published online October 16, 2025.  [Content Brief]