egfr-in-16

EGFR-IN-16 (AG473) is an inhibitor of EGFR in human A431 cells.

EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of the L858R/T790M/C797S mutant EGFR kinase, with an IC50 value of 0.87 nM. EGFR-IN-161 effectively inhibits tumor cell apoptosis, G1 phase arrest, and migration.

EGFR-IN-162 (compound 20) is an effective EGFR inhibitor that enhances both early and late apoptosis (EGFR) as well as necrosis (necrosis). It shows potential for use in breast cancer research.

EGFR-IN-160 is an EGFR inhibitor with IC50 values of 1.62, 0.49, and 0.98 μM for EGFRWT, EGFRT790M, and EGFRL858R/T790M/C797S, respectively. It can induce cell cycle arrest at the G2/M and S phases and apoptosis (Apoptosis) in NCI-H522 cells, demonstrating anticancer properties. Additionally, EGFR-IN-160 exhibits antioxidant activity against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM).

EGFR-IN-164 (Compound 4) is a selective covalent allosteric inhibitor of EGFR. It effectively inhibits the activity of EGFR^L858R/T790M/C797S kinase with an IC50 of 48.1 nM and suppresses the proliferation of EGFR-mutant cells. EGFR-IN-164 is applicable in research focused on cancer resistance.

EGFR-IN-163 (Compound 13) is a competitive inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.079 μM and selective inhibition on HER-2. It induces apoptosis in tumor cells and causes cell cycle arrest at the G₂/M phase. EGFR-IN-163 shows promise for investigating estrogen receptor-positive (ER+) breast cancer.

EGFR-IN-165 is a potent EGFR inhibitor with IC50 values of 17.18 nM for EGFRL858R/T790M kinase and 64.74 nM for EGFRWT. Its IC50 values for NCI-H1975 and A431 cell lines are 2.17 μM and 6.2 μM, respectively. EGFR-IN-165 significantly inhibits cell migration, induces G1 phase cell cycle arrest, and causes apoptosis. It is suitable for research on cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma.

EGFR-IN-1671 is a selective EGFR inhibitor with an IC50 value of 0.19 nM. It effectively inhibits various EGFR mutants, showing IC50 values of 0.109 nM for EGFR(L858R), 0.75 nM for EGFR(C797S), and less than 0.05 nM for EGFR(del19). EGFR-IN-1671 covalently binds to the catalytically conserved lysine of EGFR in live mammalian cells. By inhibiting EGFR autophosphorylation, this compound demonstrates excellent antiproliferative activity. EGFR-IN-1671 is applicable in research on non-small cell lung cancer (NSCLC), glioblastoma, and various solid tumors.

EGFR-IN-168 (Compound 9a) is a potent EGFR inhibitor with an IC50 of 0.069 μM and demonstrates antitumor activity.

EGFR-IN-166 (Compound 2) is an EGFR inhibitor demonstrating potent anticancer activity against breast cancer cells, with an IC50 of 69.63 μM for MCF-7 cells and 22.84 μM for MDA-MB-231 cells. It notably inhibits cell migration and EGFR expression, making it valuable for breast cancer research.

EGFR-IN-169 is an epidermal growth factor receptor (EGFR) inhibitor derived from ginsenoside, with an IC50 of 5.19 μM. It disrupts colorectal cancer cell migration and growth by inhibiting the EGFR-mediated RalA/EMT pathway. With an IC50 of 4.46 μM against HCT-116 cells and a selectivity index (SI) of 16.92, EGFR-IN-169 also inhibits CDKs, induces G0/G1 cell cycle arrest, and suppresses cell migration and invasion. Additionally, EGFR-IN-169 reduces mitochondrial membrane potential, induces apoptosis and reactive oxygen species (ROS) production. It is applicable in cancer research, particularly for colorectal cancer.

EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM), exhibiting antitumor activity. This compound inhibits migration of SK-BR-3 cells, arrests the cell cycle in the G0/G1 phase, and induces cell apoptosis (apoptosis). Demonstrating strong antiproliferative properties in tumor cell models with minimal damage to healthy cells, EGFR/HER2-IN-16 shows promise for research in breast cancer treatments.