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-P9912A
    Pertuzumab (anti-HER2)
    Inhibitor 99.10%
    Pertuzumab (anti-HER2), a humanized monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.
    Pertuzumab (anti-HER2)
  • 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-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-15644
    Tyrphostin 23
    Inhibitor 98.19%
    Tyrphostin 23 (Tyrphostin A23) is an EGFR inhibitor with an IC50 and Kiof 35 and 11 μM, respectively.
    Tyrphostin 23
  • 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-112411
    PD 174265
    Inhibitor 98.35%
    PD 174265 is a potent, cell-permeable, reversible, and selective inhibitor of EGFR with an IC50 of 450 pM.
    PD 174265
  • HY-13314
    Tesevatinib
    Inhibitor 99.41%
    Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity.
    Tesevatinib
  • HY-P9969
    Matuzumab
    ≥99.0%
    Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth.
    Matuzumab
  • HY-100213
    EAI045
    Inhibitor 99.08%
    EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.
    EAI045
  • HY-10530
    Varlitinib
    Inhibitor 99.92%
    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-112823A
    Almonertinib mesylate
    Inhibitor 99.67%
    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-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-156698
    HJM-561
    Degrader 98.64%
    HJM-561 is a selective and effective orally active EGFR PROTAC degrader. HJM-561 is able to overcome the triple EGFR mutations that are resistant to Osimertinib (HY-15772). HJM-561 exhibits potent degradation of EGFR Del19/T790M/C797S (DC50: 9.2 nM) and L858R/T790M/C797S (DC50: 5.8 nM), and has anti-tumor activity (pink: EGFR ligand (HY-12857); blue: CRBN ligand (HY-A0003); black: linker).
    HJM-561
  • 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-50898B
    Lapatinib ditosylate monohydrate
    Inhibitor 99.99%
    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-15164
    Icotinib Hydrochloride
    Inhibitor 99.89%
    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-109189
    Rezivertinib
    Inhibitor 99.62%
    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-14596R
    Genistein (Standard)
    Inhibitor 99.31%
    Genistein (Standard) is the analytical standard of Genistein. This product is intended for research and analytical applications. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
    Genistein (Standard)
  • 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-10045
    AEE788
    Inhibitor 99.13%
    AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.
    AEE788
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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