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-P991243
    MP-RM-1
    Inhibitor
    MP-RM-1 is a selective murine monoclonal antibody inhibitor targeting human epidermal growth factor receptor 3 (ErbB-3). MP-RM-1 blocks the activation of ErbB-3 induced by neuregulin 1 (NRG-1β) and promotes the internalization and degradation of ErbB-3, inhibiting downstream signaling pathways such as PI3K-Akt. MP-RM-1 is promising for research of ErbB-3 highly expressed solid tumors such as breast cancer, melanoma, and prostate cancer.
    MP-RM-1
  • HY-174826
    EGFR-IN-164
    Inhibitor
    EGFR-IN-164 (Compound 4) is a selective and covalent allosteric EGFR inhibitor. EGFR-IN-164 significantly inhibits the activity of EGFRL858R/T790M/C797S kinase (IC50: 48.1 nM) and proliferation of of EGFR-mutant cells. EGFR-IN-164 can be used for drug resistance of cancer research.
    EGFR-IN-164
  • HY-18963R
    Lavendustin A (Standard)
    Inhibitor
    Lavendustin A (Standard) is the analytical standard of Lavendustin A. This product is intended for research and analytical applications. Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis[1][2].
    Lavendustin A (Standard)
  • HY-E70696
    EGFR C797S/L858R 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 C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR C797S/L858R protein that can be used to study EGFR C797S/L858R-related functions.
    EGFR C797S/L858R Recombinant Human Active Protein Kinase
  • HY-143733
    HER2-IN-5
    Inhibitor
    HER2-IN-5 is a potent and orally active HER-2 inhibitor, example 10, extracted from patent WO2021164697.
    HER2-IN-5
  • HY-172091
    CZY43
    Degrader
    CZY43 is a HER3 degrader. CZY43 can effectively induce HER3 degradation in a dose- and time-dependent manner in breast cancer SKBR3 cells. CZY43 potently inhibits HER3-dependent signaling and cancer cell growth and outperforms Bosutinib (HY-10158).
    CZY43
  • HY-144053
    EGFR-IN-36
    Inhibitor
    EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research.
    EGFR-IN-36
  • HY-120412
    SKLB188
    Inhibitor
    SKLB188 is an orally active and potent epidermal growth factor receptor (EGFR) inhibitor (IC50=5 nM). SKLB188 suppresses MEK/Erk and Akt/mTOR signaling pathways to inhibit head and neck squamous cell carcinoma (HNSCC) proliferation and induce caspase-dependent apoptosis. SKLB188 is promising for research of EGFR-overexpressing solid tumors.
    SKLB188
  • HY-16558R
    Butein (Standard)
    Inhibitor
    Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
    Butein (Standard)
  • HY-B0794BR
    AZ7550 Mesylate (Standard)
    Inhibitor
    AZ7550 Mesylate (Standard) is the analytical standard of AZ7550 Mesylate. This product is intended for research and analytical applications. AZ7550 Mesylate is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
    AZ7550 Mesylate (Standard)
  • HY-50898S3
    Lapatinib-d4-1
    Inhibitor
    Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
    Lapatinib-d<sub>4</sub>-1
  • HY-179031
    EGFR/VEGFR2-IN-7
    Inhibitor
    EGFR/VEGFR2-IN-7 (Compound 3e) is a dual-target EGFR/VEGFR2 inhibitor, with IC50 values of 142 (EGFR) and 71 nM (VEGFR2). EGFR/VEGFR2-IN-7 exhibits broad-spectrum and potent anti-proliferative activity, especially being sensitive to breast cancer. EGFR/VEGFR2-IN-7 induces cell cycle arrest and apoptosis, inhibits cell migration and invasion. EGFR/VEGFR2-IN-7 can be used for research on breast cancer.
    EGFR/VEGFR2-IN-7
  • HY-147802
    EGFR-IN-59
    Inhibitor
    EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC50=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer.
    EGFR-IN-59
  • HY-142517
    EGFR-IN-25
    Inhibitor
    EGFR-IN-25 is a potent EGFR inhibitor with IC50s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively.
    EGFR-IN-25
  • HY-174414
    EGFR/HER2-IN-18
    Inhibitor
    EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC50 values of 0.09 (EGFR) and 0.08 μM (HER2) respectively. EGFR/HER2-IN-18 exhibits broad-spectrum anti-cancer activity. EGFR/HER2-IN-18 induces MCF-7 cells apoptosis and inhibits the cell cycle. EGFR/HER2-IN-18 can be used for the study of breast cancer.
    EGFR/HER2-IN-18
  • HY-155079A
    (R)-DZD1516
    Control 98.80%
    (R)-DZD1516 is the R enantiomer of DZD1516 (HY-155079). DZD1516 is a potent and selective HER2 inhibitor.
    (R)-DZD1516
  • HY-E70698
    EGFR d746-750/C797S 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 d746-750/C797S Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/C797S protein that can be used to study EGFR d746-750/C797S-related functions.
    EGFR d746-750/C797S Recombinant Human Active Protein Kinase
  • HY-175171
    Anticancer agent 276
    Inhibitor
    Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC50s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα.
    Anticancer agent 276
  • HY-101960
    (Z)-Tyrphostin A51
    Inhibitor
    (Z)-Tyrphostin A51 is the Z configuration of Lanoconazole A51. Tyrphostin A51 is a potent protein tyrosine kinase (PTK) inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [3H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation.
    (Z)-Tyrphostin A51
  • HY-176788
    EGFR Ligand-Linker Conjugates 1
    Inhibitor
    EGFR Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for EGFR (HY-150905) and a PROTAC linker, which recruits E3 ligases. EGFR Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC EGFR degrader 3 (HY-144605).
    EGFR Ligand-Linker Conjugates 1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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