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-112823A
    Almonertinib mesylate
    		Inhibitor 99.16%
    Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer.
    Almonertinib mesylate
  • HY-P9969
    Matuzumab
    		98.12%
    Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth.
    Matuzumab
  • HY-15164
    Icotinib Hydrochloride
    		Inhibitor 99.81%
    Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q. Icotinib (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.
    Icotinib Hydrochloride
  • HY-P9964
    Necitumumab
    		Inhibitor 99.51%
    Necitumumab is a human IgG monoclonal antibody directed against EGFR. Necitumumab can be used for research of NSCLC, colorectal cancer, etc.
    Necitumumab
  • HY-P99849
    Depatuxizumab
    		Inhibitor 99.58%
    Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer.
    Depatuxizumab
  • HY-10530
    Varlitinib
    		Inhibitor 98.03%
    Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.
    Varlitinib
  • HY-12026
    WZ4002
    		Inhibitor 98.99%
    WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFRL858R, EGFRL858R/T790M, EGFRE746_A750 and EGFRE746_A750/T790M, respectively.
    WZ4002
  • HY-13896
    PD168393
    		Inhibitor 98.58%
    PD168393?is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC.
    PD168393
  • HY-10333
    BMS-690514
    		Inhibitor 99.07%
    BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
    BMS-690514
  • HY-18609
    PD158780
    		Inhibitor 99.56%
    PD158780 is a potent EGFR family inhibitor with IC50s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.
    PD158780
  • HY-112411
    PD 174265
    		Inhibitor 98.72%
    PD 174265 is a potent, cell-permeable, reversible, and selective inhibitor of EGFR with an IC50 of 450 pM.
    PD 174265
  • HY-50898B
    Lapatinib ditosylate monohydrate
    		Inhibitor 99.93%
    Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) 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 ditosylate monohydrate
  • HY-10045
    AEE788
    		Inhibitor 99.13%
    AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.
    AEE788
  • HY-112299
    Zipalertinib
    		Inhibitor 99.81%
    Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM.
    Zipalertinib
  • HY-12872
    Nazartinib
    		Inhibitor 99.03%
    Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.
    Nazartinib
  • HY-108052
    Delphinidin 3-glucoside chloride
    		Inhibitor 99.89%
    Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL). Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC50 of 9.7 μM. Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC50 of 2.37 µM. Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction.
    Delphinidin 3-glucoside chloride
  • HY-141676
    HyT36
    		Degrader
    HyT36 is a low molecular weight hydrophobic tag that promotes the degradation of fusion protein and pseudokinase Her3.
    HyT36
  • HY-P99304
    Lumretuzumab
    		Inhibitor ≥99.0%
    Lumretuzumab (Anti-Human ERBB3 Recombinant Antibody) is a humanized anti-HER3 (ERBB3) monoclonal antibody that can be used for the research of cancer.
    Lumretuzumab
  • HY-109189
    Rezivertinib
    		Inhibitor 99.43%
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
    Rezivertinib
  • HY-147183B
    JBJ-09-063 hydrochloride
    		Inhibitor 99.37%
    JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer.
    JBJ-09-063 hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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