egfrin11

EGFR-IN-11 is a selective inhibitor of EGFR-tyrosine kinase and induces cell apoptosis. EGFR-IN-11 inhibits triple mutant EGFRL858R/T790M/C797S with an IC50 of 18 nM and arrests cell cycle at G0/G1.

EGFR-IN-110 (Compound 6) is a covalent inhibitor of EGFR, demonstrating pIC50 values of 9.2 for the EGFR enzyme and 8.7 for EGFR cells. It exhibits strong efficacy in targeting EGFR and maintains good kinase selectivity.

EGFR-IN-116 (compound 14D) is an antineoplastic agent. It exhibits an IC50 value of 0.103 μM for EGFR, 0.069 μM for VEGFR-2, and 19.74 μM for Topo II.

EGFR-IN-115 (H-13) is an EGFR inhibitor with an IC50 value of 395.2 nM and is applicable in cancer research.

EGFR-IN-118 (Compound 4a) is an inhibitor of the tyrosine kinase EGFR. It exhibits anticancer properties, effectively inhibiting the proliferation of MCF-7 and PC3 cells, with IC50 values of 2.53 and 3.25 µg/ml, respectively. Additionally, EGFR-IN-118 demonstrates antioxidant activity by inhibiting DPPH free radicals, with an IC50 of 10.04 µg/ml.

EGFR-IN-112 (SPP10), an EGFR kinase inhibitor, displays IC50 values of 2.31 ± 0.3 μM for MCF-7, 3.16 ± 0.8 μM for H69AR, and 4.2 ± 0.2 μM for PC-3 cancer cells, showcasing selective cytotoxicity towards these cancer cell lines.

EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutations, specifically targeting the tumor environment and inducing apoptosis in cancer cells. This compound effectively inhibits the proliferation of H1975, PC-9, and mutant EGFR cells including BaF3-EGFRL858R/T790M/C797S and BaF3–C797S/Del19/T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM respectively. Additionally, EGFR-IN-117 demonstrates anti-tumor activity in mouse models.

EGFR-IN-119 (Compound 5l) functions as an inhibitor of EGFR with an IC50 of 84.3 nM. It exhibits cytotoxic effects in A549 lung cancer cells with an IC50 of 1.34 μM. Additionally, EGFR-IN-119 downregulates the expression of EGFR, KRAS, and MAP2K genes. It displays antioxidative activity by decreasing reactive oxygen species (ROS) and hyperpolarizing mitochondrial membrane potential.