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-170543
    Dual Galectin-3/EGFR-IN-1
    Inhibitor
    Dual Galectin-3/EGFR-IN-1 (Compound 29) is the dual inhibitor for Galectin-3 and EGFR with the KD of 52.29 μM and 3.31 μM. Dual Galectin-3/EGFR-IN-1 inhibits TGF-β-induced hepatic stellate cell (HSCs) activation, induces apoptosis in LX-2 cell, and exhibits anti-liver fibrotic efficacy.
    Dual Galectin-3/EGFR-IN-1
  • HY-173314
    EGFR-IN-155
    Inhibitor
    EGFR-IN-155 (compound 13a) is an EGFR inhibitor with IC50 values of 0.14 nM and 0.18 nM against EGFR TK and EGFR L858R, respectively. EGFR-IN-155 inhibits tumor growth, causes a cell cycle arrest at S phase, and and induces cell apoptosis.
    EGFR-IN-155
  • HY-162300
    EGFR kinase inhibitor 4
    Inhibitor
    EGFR kinase inhibitor 4 (Compound 4) is a bivalent ATP-allosteric EGFR inhibitor (IC50: 1.8 nM for mutant EGFR (LRTMCS)). EGFR kinase inhibitor 4 can be used for research of NSCLC.
    EGFR kinase inhibitor 4
  • HY-144097
    HER2-IN-8
    Inhibitor
    HER2-IN-8 is a HER-2 inhibitor extracted from patent WO2021179274A1 compound 107. HER2-IN-8 can be used for the research of cancer and inflammation.
    HER2-IN-8
  • HY-E70703
    EGFR d752-759 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 d752-759 Recombinant Human Active Protein Kinase is a recombinant EGFR d752-759 protein that can be used to study EGFR d752-759-related functions.
    EGFR d752-759 Recombinant Human Active Protein Kinase
  • HY-P11078
    LARLLT
    LARLLT (D4) is an EGFR-binding peptide. LARLLT has the potential for research of EGFR overexpressing cancers, such as lung, ovarian and colorectal cancer.
    LARLLT
  • HY-172111
    EGFR-IN-144
    Inhibitor
    EGFR-IN-144 (Compound 4B) exhibits inhibitory activities against EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). EGFR-IN-144 exhibits cytotoxicity in multiple cancer cell with GI50 of nanomolare levels. EGFR-IN-144 downregulates the expressions of mTOR, TNF-α, and IL-6, arrests the cell cycle at G1/S phase, and induces apoptosis.
    EGFR-IN-144
  • HY-168173
    EGFR-IN-130
    Inhibitor
    EGFR-IN-130 (compound 14b) is an EGFR inhibitor and apoptosis inducer. EGFR-IN-130 triggers death of HeLa cancer cells via apoptosis induction..
    EGFR-IN-130
  • HY-178157
    Multi-target kinase-IN-7
    Inhibitor
    Multi-target kinase-IN-7 (Compound 1e) is an orally active multi-target kinase inhibitor (IC50 values: CDK2=0.314 μM, EGFR=0.183 μM, HER-2=0.197 μM, VEGFR-2=0.235 μM). Multi-target kinase-IN-7 is promising for research of solid tumors (e.g., lung, breast, prostate cancer).
    Multi-target kinase-IN-7
  • HY-144794
    EGFR-IN-46
    Inhibitor
    EGFR-IN-46 is a potent EGFR and FAK dual inhibitor with IC50s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis.
    EGFR-IN-46
  • HY-163453
    HER2-IN-19
    Inhibitor
    HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR with IC50 values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitory activity against tumor cells, IC50NCI-N87 = 1.63 nM, IC50BT474= 15.17 nM, IC50BaF3-HER2YVMA = 1.49 nM.
    HER2-IN-19
  • HY-12008S1
    Erlotinib-13C6 hydrochloride
    Erlotinib-13C6 hydrochloride is the 13C labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib-13C6 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib-<sup>13</sup>C<sub>6</sub> hydrochloride
  • HY-P99155A
    Zalutumumab (powder)
    Inhibitor
    Zalutumumab (powder) is a high affinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab (powder) binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab (powder) binds with IgG and its Fab fragment with EC50s of 7 and 19 nM, respectively. Zalutumumab (powder) can be used for the research of cancer.
    Zalutumumab (powder)
  • HY-W008914
    (E/Z)-CP-724714
    Inhibitor
    (E/Z)-CP-724714 is a racemic compound of (E)-CP-724714 and (Z)-CP-724714 isomers. CP-724714 is a potent and selective orally active ErbB2 (HER2) inhibitor.
    (E/Z)-CP-724714
  • HY-131710
    PDE5-IN-3
    Inhibitor
    PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity.
    PDE5-IN-3
  • HY-P991245
    Anti-ERBB3/HER3 (SGP1)
    Inhibitor
    Anti-ERBB3/HER3 (SGP1) is a human monoclonal antibody (mAb) targeting ERBB3/HER3. Anti-ERBB3/HER3 (SGP1) inhibits Neuregulin stimulated growth of cultured breast cancer cells. Anti-ERBB3/HER3 (SGP1) can be used in breast cancer research.
    Anti-ERBB3/HER3 (SGP1)
  • HY-149518
    EGFR/BRAFV600E-IN-3
    Inhibitor
    EGFR/BRAFV600E-IN-3 is a EGFR, BRAFV600E and EGFRT790M inhibitor with IC50 value of 57 nM, 68 nM and 9.70 nM. EGFR/BRAFV600E-IN-3 is an apoptotic inducer and also displays promising antioxidant activity.
    EGFR/BRAFV600E-IN-3
  • HY-157994
    EGFR WT/T790M-IN-2
    Inhibitor
    EGFR WT/T790M-IN-2 (Compound 7c) is a EGFR T790M/WT inhibitor with IC50 values of 0.08 and 0.13 μM, respectively. EGFR WT/T790M-IN-2 induces apoptosis by blocking the G0-G1 phase (apoptosis). EGFR WT/T790M-IN-2 has antitumor activity.
    EGFR WT/T790M-IN-2
  • HY-168433
    LSD1/EGFR-IN-1
    Inhibitor
    LSD1/EGFR-IN-1 (compound L-1) is a potent inhibitor of LSD1, EGFRT790M/L858R and EGFRL858R/T790M/C797S, with IC50s of 6.24 and 2.06 and 5.01 μM, respectively. LSD1/EGFR-IN-1 plays an important role in cancer research.
    LSD1/EGFR-IN-1
  • HY-147967
    EGFR-IN-63
    Inhibitor
    EGFR-IN-63 is an EGFR inhibition (IC50: 0.096 μM) and it has anticancer activity in MCF-7 cells (IC50: 2.49 μM).
    EGFR-IN-63
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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