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-161319
    EGFR-IN-104
    		Inhibitor
    EGFR-IN-104 (Compound A23) is an effective inhibitor of EGFR, with IC50 values of 0.33 μM and 0.133 μM against EGFRL858R/T790M and EGFRDel19/T790M/C797S, respectively. EGFR-IN-104 exhibits anticancer activity both in vitro and in vivo.
    EGFR-IN-104
  • HY-P991240
    CDX-3379
    		Inhibitor
    CDX-3379 is a humanized monoclonal antibody inhibitor targeting ErbB3. CDX-3379 binds to ErbB3, blocking the dimerization of ErbB3 with other receptors, thereby inhibiting the phosphorylation of ErbB3. CDX-3379 can inhibit the growth and proliferation of tumor cells. CDX-3379 is promising for research of tumors expressing ErbB3 and NRG1, such as HNSCC.
    CDX-3379
  • HY-168170
    EGFR/VEGFR2-IN-2
    		Inhibitor
    EGFR/VEGFR2-IN-2 (compound 4b) is an dual inhibitor VEGFR-2 and EGFR..
    EGFR/VEGFR2-IN-2
  • HY-170497
    EGFR-IN-140
    		Inhibitor
    EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with Ki of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC50 of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model.
    EGFR-IN-140
  • HY-158018
    EGFR-TK-IN-2
    		Inhibitor
    EGFR-TK-IN-2 (compound 10b) is EGFR-TK inhibitor with the IC50 of 0.16 μM. EGFR-TK-IN-2 inhibits cell growth.
    EGFR-TK-IN-2
  • HY-P991571
    GC1118
    GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer.
    GC1118
  • HY-177380
    EGFR ligand-14-PEG3-Boc
    EGFR ligand-14-PEG3-Boc contains EGFR ligand and linker. EGFR ligand-14-PEG3-Boc can be used for the synthesis of SJF-1521 (HY-131865).
    EGFR ligand-14-PEG3-Boc
  • HY-147797
    EGFR/HER2/CDK9-IN-2
    		Inhibitor
    EGFR/HER2/CDK9-IN-2 (Compound 9) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 145.35, 129.07, and 117.13 nM, respectively. EGFR/HER2/CDK9-IN-2 exhibits remarkable antitumor activity.
    EGFR/HER2/CDK9-IN-2
  • HY-175837
    EGFR-IN-172
    		Inhibitor
    EGFR-IN-172 is a EGFR inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC.
    EGFR-IN-172
  • HY-149275
    PKM2/PDK1-IN-1
    		Inhibitor
    PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway.
    PKM2/PDK1-IN-1
  • HY-156097
    Anticancer agent 158
    		Inhibitor
    Anticancer agent 158 (compound 7c) is a potent anticancer agent. The IC50s for inhibiting HepG-2, MDA-MB-231, and HCT-116 cell lines are 7.93 μM, 9.28 μM, 13.28 μM, and 181.89 μM, respectively.
    Anticancer agent 158
  • HY-164489
    KU004
    		Inhibitor
    KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative.
    KU004
  • HY-158177
    EGFR T790M/L858R-IN-6
    		Inhibitor
    EGFR T790M/L858R-IN-6 (compound 53), a pyrimidine compound, is a potent EGFR T790M/L858R inhibitor. EGFR T790M/L858R-IN-6 shows 90.88% enzyme activity inhibition with 0.05 μM.
    EGFR T790M/L858R-IN-6
  • HY-50896S1
    Erlotinib-13C6
    		Inhibitor
    Erlotinib-13C6 is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR.
    Erlotinib-<sup>13</sup>C<sub>6</sub>
  • HY-E70709
    EGFR T790M Recombinant Human Active Protein Kinase
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR T790M Recombinant Human Active Protein Kinase is a recombinant EEGFR T790M protein that can be used to study EGFR T790M-related functions.
    EGFR T790M Recombinant Human Active Protein Kinase
  • HY-106204
    Nelipepimut-S
    Nelipepimut-S is a peptide vaccine which targets HER2. Nelipepimut-S has immune activity against HER2 positive breast cancer.
    Nelipepimut-S
  • HY-168469
    EGFR-IN-148
    		Inhibitor
    EGFR-IN-148 (compound 8c) is a potent inhibitor of EGFR , with the IC50 of 0.161 μM. EGFR-IN-148 causes G1/S arrest and markedly enhances apoptosis in HepG2 cells.
    EGFR-IN-148
  • HY-150782
    UNC-CA359
    		Inhibitor
    UNC-CA359 is a potent epidermal growth factor receptor (EGFR) inhibitor, with an IC50 value of 18 nM. UNC-CA359 exhibits strong anti-tumor activity, can be used to Chordoma research. UNC-CA359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    UNC-CA359
  • HY-158016
    Antiproliferative agent-49
    		Inhibitor
    Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC50 of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC50 values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS.
    Antiproliferative agent-49
  • HY-100636A
    Gefitinib N-oxide hydrochloride
    		Inhibitor
    Gefitinib N-oxide hydrochloride is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
    Gefitinib N-oxide hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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