2. Signaling Pathways
  3. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  4. EGFR

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

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The EGFR family of receptor tyrosine kinases (RTK) comprises four distinct receptors: the EGFR (also known as ErbB-1/HER1), ErbB-2 (neu, HER2), ErbB-3 (HER3) and ErbB-4 (HER4). All EGFR family members are characterized by a modular structure consisting of an extracellular ligand-binding domain, a single hydrophobic transmembrane region, and the intracellular part harbouring the highly conserved tyrosine kinase domain. The ErbB family of receptor tyrosine kinases (RTKs) couples binding of extracellular growth factor ligands to intracellular signaling pathways regulating diverse biologic responses, including proliferation, differentiation, cell motility, and survival. Ten growth factors and their ErbB specificities are: EGF, amphiregulin (AR), and TGF bind ErbB-1; betacellulin, and epiregulin bind both ErbB-1 and ErbB-4; the neuregulins (also called heregulins and Neu differentiation factors) NRG-1 and NRG-2 bind ErbB-3 and ErbB-4; and NRG-3 and NRG-4 bind ErbB-4. No known ligand binds ErbB-2. The three best characterized signaling pathways induced through ErbBs are Ras-mitogen-activated protein kinase (Ras-MAPK), phosphatidylinositol 3 kinase-protein kinase B (PI3K-PKB/Akt), and phospholipase C-protein kinase C (PLC-PKC) pathways.

EGFR Isoform Specific Products:

EGFR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-179039
    EGFR-IN-183
    		Inhibitor
    EGFR-IN-183 (Compound 5q) is an EGFR inhibitor. EGFR-IN-183 strongly binds to EGFR (T790M/L858R) mutants. EGFR-IN-183 exhibits anti-proliferative activity against MDA-MB-231, with an IC50 value of 16.4 μM. EGFR-IN-183 can be used for research on triple-negative breast cancer.
    EGFR-IN-183
  • HY-146473
    EGFR-IN-53
    		Inhibitor
    EGFR-IN-53 (Compound 7) is a potent EGFR inhibitor with an IC50 of 8.264 µM. EGFR-IN-53 shows cytotoxic activity against cancer cell lines.
    EGFR-IN-53
  • HY-171747
    AMT-562
    		Antagonist
    AMT-562 is an antibody-drug conjugate (ADC) consisting of a novel anti-HER3 antibody Ab562 (HY-P991505) conjugated to the linker Mc-VC-PAB and the topoisomerase I inhibitor Exatecan (HY-13631). The ADC toxic molecule and linker portion are MC-VA-PAB-Exatecan (HY-147270). AMT-562 can induce apoptosis and has antitumor activity against pancreatic, esophageal, and gastric cancers.
    AMT-562
  • HY-N3634
    Corylifol C
    Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively.
    Corylifol C
  • HY-146471
    EGFR-IN-51
    		Inhibitor
    EGFR-IN-51 (Compound 6) is a potent EGFR inhibitor with IC50 values of 0.493, 102.60 and 461.63 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-51 shows cytotoxic activity against cancer cell lines and induces apoptosis.
    EGFR-IN-51
  • HY-156457
    EGFR-IN-90
    		Inhibitor
    EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model.
    EGFR-IN-90
  • HY-168559
    EGFR-IN-131
    		Inhibitor
    EGFR-IN-131 (compound 3a) is a potent and cross the blood-brain barrier EGFR inhibitor with an IC50 value of 272.9 nM. EGFR-IN-131 shows antiproliferative activity. EGFR-IN-131 induces apoptosis and cell cycle arrest at G0/G1 phase. EGFR-IN-131 decreases the protein expression of p-EGFR.
    EGFR-IN-131
  • HY-155227S
    ALK/EGFR-IN-1-d5
    		Inhibitor
    ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment
    ALK/EGFR-IN-1-d5
  • HY-175009
    MRC-G-001
    		Inhibitor
    MRC-G-001 is a Genipin (HY-17389) derivative with an IC50 of 117 μM against A549 cancer cells. MRC-G-001 inhibits the phosphorylation of EGFR, JAK1, and STAT3, and modulates epithelial-mesenchymal transition (EMT)-related protein expression, thereby attenuating cell migration and invasion. MRC-G-001 induces cell cycle arrest and cell apoptosis. MRC-G-001 can be used for the study of cancers such as non-small-cell lung cancer.
    MRC-G-001
  • HY-147860
    EGFR-IN-61
    		Inhibitor
    EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively.
    EGFR-IN-61
  • HY-13524A
    AG-1478 hydrochloride
    		Inhibitor
    AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV).
    AG-1478 hydrochloride
  • HY-RS04470
    Erbb3 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Erbb3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Erbb3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Erbb3 Mouse Pre-designed siRNA Set A
  • HY-19730A
    Olmutinib hydrochloride
    		Inhibitor
    Olmutinib hydrochloride is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib hydrochloride is used for NSCLC.
    Olmutinib hydrochloride
  • HY-173164
    EGFR/BRAFV600E-IN-4
    		Inhibitor
    EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAFV600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity.
    EGFR/BRAFV600E-IN-4
  • HY-159512
    EGFR kinase inhibitor 7
    		Inhibitor
    EGFR kinase inhibitor 7 (compound 18i) is an EGFR inhibitor (IC50=42.3 nM) with anticancer activity. EGFR kinase inhibitor 7 has significant in vitro cytotoxicity and apoptosis induction ability. EGFR kinase inhibitor 7 has antiproliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values ​​of 4.82 µM and 1.43 µM, respectively.
    EGFR kinase inhibitor 7
  • HY-175316
    EGFR-IN-168
    		Inhibitor
    EGFR-IN-168 (Compound 9a) is a potent EGFR inhibitor with an IC50 of 0.069 μM. EGFR-IN-168 has antitumor activity.
    EGFR-IN-168
  • HY-161603
    EGFR/HER2-IN-14
    		Inhibitor
    EGFR/HER2-IN-14 (Compd 46) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research.
    EGFR/HER2-IN-14
  • HY-P10792
    HER2-targeted peptide H6F
    HER2-targeted peptide H6F is a HER2 targeting peptide that binds to HER2 to target breast cancer cells, with the amino acid sequence YLFFVFER. The HER2-targeted peptide H6F can be conjugated with the bifunctional chelating agent hydrazinonicotinamide (HYNIC) for radiolabeling with 99mTc. Single-photon emission computed tomography (SPECT) imaging shows that the labeled HER2-targeted peptide H6F specifically accumulates in HER2-positive MDA-MBA-453 tumor-bearing mice models. The HER2-targeted peptide H6F can be used for tumor molecular imaging studies.
    HER2-targeted peptide H6F
  • HY-10368
    EGFR/VEGFR2-IN-4
    		Inhibitor
    EGFR/VEGFR2-IN-4 (Compound 19) is the irreversible inhibitor for EGFR and VEGFR-2 with IC50 of 18.7 nM and 102.3 nM, under the presence of 1 μM ATP.
    EGFR/VEGFR2-IN-4
  • HY-P990408
    Anti-ERBB1/EGFR/HER1 Antibody
    		Inhibitor
    The Anti-ERBB1/EGFR/HER1 Antibody is a CHO-expressed human antibody that targets ERBB1/EGFR/HER1. The Anti-ERBB1/EGFR/HER1 Antibody consists of a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for the Anti-ERBB1/EGFR/HER1 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-ERBB1/EGFR/HER1 Antibody
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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