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-146423
    PROTAC EGFR degrader 6
    		Inhibitor
    PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase.
    PROTAC EGFR degrader 6
  • HY-163723
    EGFR-IN-116
    		Inhibitor
    EGFR-IN-116 (compound 14D) is an anticancer agent. EGFR-IN-116 against EGFR has the IC50 values​of EGFR, VEGFR-2 and Topo II are 0.103 μM, 0.069 μM and 19.74 μM, respectively.
    EGFR-IN-116
  • HY-108052R
    Delphinidin 3-glucoside chloride (Standard)
    		Inhibitor
    Delphinidin 3-glucoside (chloride) (Standard) is the analytical standard of Delphinidin 3-glucoside (chloride). This product is intended for research and analytical applications. Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL). Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC50 of 9.7 μM. Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC50 of 2.37 µM. Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction.
    Delphinidin 3-glucoside chloride (Standard)
  • HY-P99500
    Cetuximab sarotalocan
    		Inhibitor
    Cetuximab sarotalocan (RM-1929) is an IRdye700DX (near-infrared photosensitizing dye) conjugate of Cetuximab (anti-EGFR monoclonal antibody). Cetuximab sarotalocan can be used for head and neck cancers research.
    Cetuximab sarotalocan
  • HY-101958
    Tyrphostin 25
    		Inhibitor 99.00%
    Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase with an IC50 value of 3 µM in A431 cells. Tyrphostin 25 is also a GPR35 agonist with an EC50 of 5.3 µM.
    Tyrphostin 25
  • HY-116138
    RG-14467
    		Inhibitor
    RG-14467 is an epidermal growth factor receptor tyrosine kinase inhibitor with activity that inhibits enzyme activity. RG-14467 has similar inhibition kinetics to Lavendustin-A, with a dissociation constant of 3.4μM for the initial rapidly formed complex and an overall dissociation constant estimated to be less than or equal to 30nM, and is a partially competitive inhibitor for ATP.
    RG-14467
  • HY-115952
    EGFR/HER2-IN-3
    		Inhibitor
    EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of EGFR and HER2.
    EGFR/HER2-IN-3
  • HY-144051
    EGFR-IN-34
    		Inhibitor
    EGFR-IN-34 is a potent inhibitor of EGFR. EGFR-IN-34 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-34 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 12).
    EGFR-IN-34
  • HY-144056
    EGFR-IN-39
    		Inhibitor
    EGFR-IN-39 is a potent inhibitor of EGFR. EGFR-IN-39 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-39 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 2).
    EGFR-IN-39
  • HY-161785
    EGFR-IN-117
    		Inhibitor
    EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFRL858R/T790M/C797S and BaF3–C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models.
    EGFR-IN-117
  • HY-143729
    EGFR-IN-29
    		Inhibitor
    EGFR-IN-29 is a potent EGFR inhibitor, example J-022, extracted from Patent WO2021160087.
    EGFR-IN-29
  • HY-160068
    2-2(t) aptamer sodium
    		Chemical
    2-2(t) aptamer sodium is a 42-nucleotide trimeric complex of aptamer (2-2) targeting ErbB-2. 2-2(t) aptamer sodium inhibits the growth of gastric cancer cells in vitro and in vivo.
    2-2(t) aptamer sodium
  • HY-155969
    EGFR-IN-83
    		Inhibitor
    EGFR-IN-83 (Compound 9) is an EGFR inhibitor (IC50: 2.53 nM). EGFR-IN-83 has antiproliferative activity against MCF-7 and MDA-MB-231 cells, with IC50 of 2.50 μM and 1.96 μM. EGFR-IN-83 can induce cell apoptosis.
    EGFR-IN-83
  • HY-P990055
    Nezutatug
    		Inhibitor
    Nezutatug is an anti-HER3 antibody, and used for cancer research.
    Nezutatug
  • HY-169309
    EGFR-IN-133
    		Inhibitor
    EGFR-IN-133 (Compound 24) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. EGFR-IN-133 exhibits good pharmacokinetics characteristics with high oral exposure.
    EGFR-IN-133
  • HY-169408
    EGFR-IN-137
    		Inhibitor
    EGFR-IN-137 (Compound 4c) is an inhibitor for aromatase and EGFR with IC50s of 1.67 μg/mL and 0.08 μg/mL. EGFR-IN-137 inhibits the proliferation of cancer cell MCF-7 and MDA-MB-231 with IC50s of 1.62 µM and 4.14 µM. EGFR-IN-137 arrests the cell cycle at G0/G1 phase in MDA-MB-231, and induces apoptosis through caspase-dependent pathway.
    EGFR-IN-137
  • HY-144054
    EGFR-IN-37
    		Inhibitor
    EGFR-IN-37 is a potent inhibitor of EGFR. EGFR-IN-37 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-37 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 7).
    EGFR-IN-37
  • HY-P5745A
    TYVPANASL TFA
    TYVPANASL TFA is a MHC I-binding CD8 T cell epitope of nine amino acids from HER2/neu. TYVPANASL TFA can be used to prepare J-LEAPS vaccine.
    TYVPANASL TFA
  • HY-173218
    anti-NSCLC agent-1
    		Inhibitor
    anti-NSCLC agent-1 (compound 8dc) is an inhibitor of tyrosine kinase inhibitors (TKIs) with IC50 values of 0.05 and 0.09 μM in A549 and NCI-H441 cells. anti-NSCLC agent-1 shows anti-NSCLC activities in colony formation, migration, and invasion.
    anti-NSCLC agent-1
  • HY-158154
    EGFR-IN-110
    		Inhibitor
    EGFR-IN-110 (Compound 6) is a covalent EGFR inhibitor, with pIC50 values of 9.2 and 8.7 for EGFR enzyme and EGFR cell, respectively. EGFR-IN-110 shows high EGFR potency and good kinase selectivity.
    EGFR-IN-110
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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