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

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-172104
    EGFR-IN-143
    Inhibitor
    EGFR-IN-143 (Compound 5f) is a potent EGFR inhibitor with an IC50 value of 0.15 μM. EGFR-IN-143 induces apoptosis by arresting the cell cycle in the G2/M phase. EGFR-IN-143 has antitumor activity.
    EGFR-IN-143
  • HY-157912
    EGFR-IN-102
    Inhibitor
    EGFR-IN-102 (compound 6) is an oral active EGFR inhibitor with the IC50 of 2 nM, and can be used for study of non-small-cell lung cancer.
    EGFR-IN-102
  • HY-141486A
    PROTAC PARP/EGFR ligand 1
    PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology.
    PROTAC PARP/EGFR ligand 1
  • HY-144049
    EGFR-IN-32
    Inhibitor
    EGFR-IN-32 is a potent inhibitor of EGFR. 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-32 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185297A1, compound 2).
    EGFR-IN-32
  • HY-163371
    EGFR WT/T790M-IN-1
    Inhibitor
    EGFR WT/T790M-IN-1 (Compound 16h) is a dual EGFR WT and EGFR T790 inhibitor. EGFR WT/T790M-IN-1 can arrest the cell cycle in G2/M phase and induce apoptosis. EGFR WT/T790M-IN-1 has anti-cancer activity.
    EGFR WT/T790M-IN-1
  • HY-177379
    EGFR ligand-14
    EGFR ligand-14 is an EGFR ligand. EGFR ligand-14 can be used for the synthesis of SJF-1521 (HY-131865).
    EGFR ligand-14
  • HY-178955
    EGFR-IN-182
    Inhibitor
    EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer.
    EGFR-IN-182
  • HY-P10686
    CH401 peptide
    CH401 peptide is a HER2-derived antigen peptide. After being bound to the artificial viral capsid by a self-assembled β-cyclic peptide, CH401 peptide is encapsulated in a lipid bilayer containing the lipid adjuvant α-GalCer, and can be studied as a self-adjuvant anti-breast cancer vaccine candidate.
    CH401 peptide
  • HY-149695
    EGFR-IN-91
    Inhibitor
    EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFRL858R/C797S and EGFRexon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants.
    EGFR-IN-91
  • HY-162483
    EGFR kinase inhibitor 6
    Inhibitor
    EGFR kinase inhibitor 6 (Compound 4b) is an orally active inhibitor for epidermal growth factor receptor (EGFR) kinase, with IC50 of 24.34 μM. EGFR kinase inhibitor 6 induces apoptosis. EGFR kinase inhibitor 6 exhibits anticancer and anti-inflammatory activity with low toxicity (LD50 range: 500-2000 mg/kg).
    EGFR kinase inhibitor 6
  • HY-118175
    RG 14921
    Inhibitor
    RG 14921 is a compound structurally related to Erbstatin (HY-113549) and has inhibitory activity against EGFR tyrosine kinase and CAMP-dependent kinase activity. RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor.
    RG 14921
  • HY-168112
    EGFR-IN-127
    Inhibitor
    EGFR-IN-127 is an ATP-competitive EGFR inhibitor with IC50s of 136.3 nM and 161. 2 nM for EGFRdel19 and EGFRdel19/T790M/C797S, respectively. EGFR-IN-127 has the potential for the study of non-small-cell lung cancer (NSCLC).
    EGFR-IN-127
  • HY-101820A
    Simotinib hydrochloride
    Inhibitor
    Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
    Simotinib hydrochloride
  • HY-173619
    EGFR-IN-160
    Inhibitor
    EGFR-IN-160 (Compound R12) is an EGFR inhibitor (IC50 values are 1.62, 0.49 and 0.98 μM for EGFRWT, EGFRT790M and EGFRL858R/T790M/C797S, respectively). EGFR-IN-160 induces G2/M and S phase arrest and apoptosis in NCI-H522 cells, and has anticancer activity. EGFR-IN-160 has antioxidant effects against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM).
    EGFR-IN-160
  • HY-P991572
    MM-151
    Antagonist
    MM-151 is a humanized IgG1 monoclonal antibody targeting EGFR. MM-151 binds multiple regions of the EGFR extracellular domain (ECD) and reduces its mutations in circulating cell-free tumor DNA with EGFR resistance. MM-151 significantly inhibits EGFR signaling and cell growth. MM-151 can be used for drug-resistant cancers research, such as colorectal, non-small cell lung and triple negative breast cancer.
    MM-151
  • HY-18298
    PD 173955 analog 1
    Inhibitor
    PD 173955 analog 1 (Compound 26) is an analog of PD 173955 (HY-10395). PD 173955 analog 1 is an inhibitor for EGFR kinase, which exhibits antitumor and toxicological properties. PD 173955 analog 1 exhibits an in silico IC50 of 0.19 μM.
    PD 173955 analog 1
  • HY-149633
    EGFR/HER2/DHFR-IN-3
    Inhibitor
    EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells.
    EGFR/HER2/DHFR-IN-3
  • HY-175173
    EGFR-IN-166
    Inhibitor
    EGFR-IN-166 (Compound 2) is a EGFR inhibitor. EGFR-IN-166 has potent anticancer activity against breast cancer cells with IC50s of 69.63 and 22.84 μM for MCF-7 and MDA-MB-231 cells, respectively. EGFR-IN-166 significantly inhibits cell migration and EGFR expression. EGFR-IN-166 can be used for breast cancer research.
    EGFR-IN-166
  • HY-146138
    EGFR-IN-57
    Inhibitor
    EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis.
    EGFR-IN-57
  • HY-162332
    EGFR-PK/JNK-2-IN-1
    Inhibitor
    EGFR-PK/JNK-2-IN-1 (Compound 6c) is a dual inhibitor of EGFR-PK and JNK-2 with IC50s of 2.7 and 3.0 μM, respectively. EGFR-PK/JNK-2-IN-1 can induce apoptosis and induce cell cycle arrest at different cell phases. EGFR-PK/JNK-2-IN-1 can be used for the research of cancer.
    EGFR-PK/JNK-2-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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