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-10530A
    Varlitinib tosylate
    Inhibitor
    Varlitinib (ASLAN001) tosylate is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.
    Varlitinib tosylate
  • HY-138746
    EGFR-IN-15
    Inhibitor
    EGFR-IN-15 (compound I-005) is a EGFR inhibitor with an IC50 of 4 nM. EGFR-IN-15 can be used for oncological diseases research.
    EGFR-IN-15
  • HY-115951
    EGFR/HER2-IN-2
    Inhibitor
    EGFR/HER2-IN-2 (Compound ZINC35560729) is a dual inhibitor of EGFR and HER2 with IC50 values of 5.02 µM and 0.83 µM against EGFR and HER2, respectively.
    EGFR/HER2-IN-2
  • HY-125841
    EGFR mutant-IN-1
    Inhibitor
    EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM).
    EGFR mutant-IN-1
  • HY-147407
    Imbotolimod
    Inhibitor
    Imbotolimod, immunoglobulin G1-kappa, is a humanized monoclonal antibody with anti-ERBB2 and antineoplastic activity. Imbotolimod is a derivative of telratolimod.
    Imbotolimod
  • HY-147303
    Sacibertinib
    Inhibitor
    Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity.
    Sacibertinib
  • HY-P990978
    Caxmotabart
    HY-P990978 is an ERBB2-targeting IgG1κ type humanized antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Caxmotabart
  • HY-P990909
    Calotatug
    HY-P990909 is an ERBB2-targeting IgG1κ type human antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Calotatug
  • HY-10407G
    SU 5402 (GMP)
    Inhibitor
    SU 5402 (GMP) is SU 5402 (HY-10407) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
    SU 5402 (GMP)
  • HY-174232
    EGFR/CA-IX-IN-1
    Inhibitor
    EGFR/CA-IX-IN-1 (Compound 14) is a dual inhibitor against epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX) with IC50 values of 5.92 nM and 63 nM, respectively. EGFR/CA-IX-IN-1 shows strong cytotoxicity against breast cancer cells (MDA-MB-231, MCF-7) with IC50 values of 5.78 μM and 8.05 μM, respectively. EGFR/CA-IX-IN-1 inhibits the catalytic activity of CA-IX, up-regulates BAX/Bcl-2, activates caspases, and arrests the cell cycle at the G1 phase. EGFR/CA-IX-IN-1 is promising for research of breast cancer.
    EGFR/CA-IX-IN-1
  • HY-RS04209
    EGFR Human Pre-designed siRNA Set A
    Inhibitor

    EGFR Human Pre-designed siRNA Set A contains three designed siRNAs for EGFR gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    EGFR Human Pre-designed siRNA Set A
  • 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-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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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