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-169427
    FRF-06-057
    		Inhibitor
    FRF-06-057 is an ATP-allosteric EGFR inhibitor against wild-type and mutant EGFR, with IC50s of 17 nM (LR/TM), 29 nM (LR/TM/CS), 220 nM (LR), > 1000 nM (WT) respectively.
    FRF-06-057
  • HY-146170
    Anticancer agent 69
    		Inhibitor
    Anticancer agent 69 (Compound 34), a potent and selective anticancer agent , potently and selectively inhibits human prostate cancer cell line PC3 (IC50=26 nM). Anticancer agent 69 increases ROS level, down-regulates EGFR and induces apoptosis.
    Anticancer agent 69
  • HY-50898S2
    Lapatinib-d5
    		Inhibitor
    Lapatinib-d5 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>5</sub>
  • HY-152019
    EGFR/C797S-IN-1
    		Inhibitor
    EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner.
    EGFR/C797S-IN-1
  • HY-146422
    PROTAC EGFR degrader 5
    		Inhibitor
    PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase.
    PROTAC EGFR degrader 5
  • HY-161731
    DS08701581
    		Inhibitor
    DS08701581 is an inhibitor of FER tyrosine kinase with IC50. DS08701581 has anti-tumor activity and oral activity.
    DS08701581
  • HY-P9968A
    Nimotuzumab (powder)
    		Inhibitor
    Nimotuzumab (powder) is a humanized IgG1 monoclonal antibody targeting EGFR with a KD value of 0.21 nM. Nimotuzumab (powder) is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab (powder), a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC).
    Nimotuzumab (powder)
  • HY-172110
    Apoptosis inducer 35
    		Inhibitor
    Apoptosis inducer 35 (Compound 6) is a multi-targeted inhibitor, that reduces the expressions of EGFR, AKT, ERK and P38-MAPKα. Apoptosis inducer 35 inhibits the proliferation of cancer cell A549 and Jurkat, arrests the cell cycle at S phase, and induces apoptosis.
    Apoptosis inducer 35
  • HY-13272S3
    Dacomitinib-d10
    		Inhibitor
    Dacomitinib-d10 is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
    Dacomitinib-d<sub>10</sub>
  • 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-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-P991232
    AMX-818
    		Inhibitor
    AMX-818 is a conditionally active, masked T cell engager (TCE) targeting HER2. AMX-818 demonstrates potent T cell cytotoxicity against HER2-positive tumor cell lines. AMX-818 can also induce tumor regression in vivo. AMX-818 is promising for research of HER2-positive solid tumors.
    AMX-818
  • 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-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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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