egfr-in-15

EGFR-IN-15 (compound I-005) is a potent EGFR inhibitor with an IC50 value of 4 nM, holding potential for oncological research applications.

EGFR-IN-154 (compound 4c) is an EGFR inhibitor with EC₀ values of 0.16 μM for EGFRDel19, 21.73 μM for EGFR WT, and 41.56 μM for EGFRL858R. This compound exhibits anticancer activity across various cancer cell lines. EGFR-IN-154 induces mitochondrial apoptosis, reduces pERK1/2 and pAkt levels, and increases pJNK and pp38 levels.

EGFR-IN-155 (compound 13a) is an EGFR inhibitor with IC50 values of 0.14 nM for EGFRTK and 0.18 nM for EGFRL858R. EGFR-IN-155 suppresses tumor growth, causes cell cycle arrest at the S phase, and induces apoptosis (cell death).

EGFR-IN-153 (Compound 5l) is an EGFR inhibitor that suppresses the proliferation of MDA-MB-231 cells with an IC50 of 0.73 μM and induces apoptosis. It is applicable for research in breast cancer.

EGFR-IN-150 is an EGFR inhibitor that effectively inhibits the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. This compound exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975 and significantly suppresses the colony formation and migration abilities of H1975 and A549 cells, while also inducing apoptosis. Additionally, EGFR-IN-150 prominently reduces tumor growth in H1975 tumor-bearing mouse CDX models. It holds promise for research related to non-small cell lung cancer.

EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. It effectively suppresses the proliferation of various lung cancer cells, with IC50 values of 11.7, 5.19, 7.32, and 1.53 μM for NCI-H1781, HCC827, NCI-H3255, and NCI-H1975, respectively. Additionally, EGFR-IN-151 hinders colony formation and cell migration in H1975, induces G1 phase cell cycle arrest, and triggers apoptosis in H1975 cells.

EGFR-IN-159 (compound 12) is a dihydropyrimidine and a potent EGFR inhibitor with an IC50 of 29.00 nM. It exhibits dose-dependent inhibition of EGFR and HER2. The compound shows cytotoxicity against MCF-7 breast cancer cells and Vero cells with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. EGFR-IN-159 does not cross the blood-brain barrier (BBB) and demonstrates significant anticancer activity.

EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC50 value of 0.22 nM for EGFR (Del19/T790M). By binding to EGFR, EGFR-IN-158 inhibits phosphorylation and downstream signaling, thereby suppressing the proliferation of tumor cell lines and promoting apoptosis.

EGFR-IN-157 (compound IIB-5) is a potent EGFR inhibitor with an IC50 of 18.81 nM and is applicable for research in non-small cell lung cancer (NSCLC).

EGFR-IN-156 (Compound 7f) is an EGFR inhibitor with inhibitory activity against mutant EGFRL858R and EGFRT790M, with IC50 values of 0.186, 0.131, and 0.107 μM, respectively. It exhibits significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer), with IC50 values of 1.67, 5.32, and 6.56 μM, respectively. EGFR-IN-156 suppresses cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. It shows potential in EGFR-related cancers.

EGFR-IN-152 (compound D4) is a potent inhibitor of the EGFR tyrosine kinase and exhibits significant inhibitory activity against the EGFRL858R/T790M/C797S mutations (IC50= 40 nM). It induces cell cycle arrest at the G0/G1 phase and apoptosis, thereby hindering the clonogenic growth and proliferation of non-small cell lung cancer (NSCLC) cells. EGFR-IN-152 is applicable for NSCLC research.

EGFR-IN-92 (compound 15) is an allosteric inhibitor targeting both T790M and L858R double-mutated EGFR. It exhibits antiproliferative activity against H1975 non-small cell lung cancer (NSCLC) cells expressing these double mutations.

EGFR/HER2-IN-15 is a dihydropyrimidine and an effective inhibitor of EGFR/HER2. It significantly suppresses EGFRwt activity with an IC50 of 37.21 nM and exhibits anticancer properties.

EGFR/InhA-IN-1 (Compound 15) is an inhibitor targeting the anticancer enzyme EGFR tyrosine kinase (1M17) with a Ki of 0.05 μM and the antituberculosis enzyme InhA (1OUZ) with a Ki of 0.02 μM. It exhibits antiproliferative activity against A549 cells (IC50 = 10.38 μM) and inhibits Mycobacterium tuberculosis H37Rv with a MIC of 6.25 μM. This compound can be utilized in studies related to non-small cell lung cancer and Mycobacterium tuberculosis infections.

PROTACEGFRdegrader 15 is a bifunctional EGFR PROTAC degrader composed of Pomalidomide and Gefitinib. It facilitates EGFR degradation through ubiquitin-proteasome dependent proteolysis and autophagic-lysosomal pathways. Additionally, PROTACEGFRdegrader 15 targets ETFA to enhance ATP production. It significantly suppresses tumor growth in Gefitinib-resistant HCC-827 xenograft models.

EGFRvIII peptide, a synthetic peptide mirroring the EGFRvIII fusion junction—a tumor-specific, perpetually active EGFR variant missing amino acids 6-273 of the wild-type—binds to HLA-A*0201-positive T2 cells under MHC class I at 25 µg/ml. It enables antigen presentation in dendritic cells from human peripheral blood mononuclear cells (PBMCs), thus activating CD8+ cytotoxic T lymphocytes and prompting IFN-γ production. Administered at 15 µg/animal with the TLR5 agonist flagellin B, EGFRvIII peptide elevates CD8+ T cell numbers, lowers regulatory T cells (Tregs) in the brain, diminishes tumor volume, and extends survival in a GL261 glioblastoma mouse model.

EGFR-IN-121 (compound 15) acts as a dual inhibitor for EGFR and VEGFR-2, with IC50 values of 84 nM and 3.5 nM, respectively.