1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  3. EGFR

EGFR

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/ErbB1/HER1

  • ErbB2/HER2

  • ErbB3/HER3

  • ErbB4/HER4

EGFR Related Products (120):

Cat. No. Product Name Effect Purity
  • HY-15772
    Osimertinib Inhibitor 99.95%
    Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
  • HY-50895
    Gefitinib Inhibitor 99.94%
    Gefitinib (ZD1839) is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
  • HY-10261
    Afatinib Inhibitor 99.99%
    Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
  • HY-50896
    Erlotinib Inhibitor 99.99%
    Erlotinib is a medication for the treatment of non-small cell lung cancer. It inhibits purified EGFR kinase with an IC50 of 2 nM.
  • HY-12000
    AG-490 Inhibitor 99.84%
    AG-490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
  • HY-P9912
    Pertuzumab Inhibitor 99.10%
    Pertuzumab, a humanized monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.
  • HY-123921
    Gefitinib-based PROTAC 3 Inhibitor 99.98%
    Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.
  • HY-100848
    TX1-85-1 Inhibitor >98.0%
    TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM and is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
  • HY-P9907
    Trastuzumab Inhibitor 99.30%
    Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.
  • HY-50898
    Lapatinib Inhibitor 99.83%
    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.
  • HY-P9905
    Cetuximab Inhibitor 99.70%
    Cetuximab is a monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for soluble EGFR by SPR. Cetuximab has potent antitumor activity.
  • HY-32721
    Neratinib Inhibitor 98.84%
    Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
  • HY-14596
    Genistein Inhibitor 99.68%
    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.
  • HY-13524
    AG-1478 Inhibitor 99.74%
    AG-1478 is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM.
  • HY-12008
    Erlotinib Hydrochloride Inhibitor 99.99%
    Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM.
  • HY-13272
    Dacomitinib Inhibitor 99.83%
    Dacomitinib 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.
  • HY-15772A
    Osimertinib mesylate Inhibitor 99.96%
    Osimertinib mesylate (AZD-9291 mesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
  • HY-15730
    Poziotinib Inhibitor 99.96%
    Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFRwt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFRT790M and EGFRL858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity.
  • HY-13050
    Sapitinib Inhibitor 99.99%
    Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
  • HY-112299
    TAS6417 Inhibitor 99.55%
    TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
Isoform Specific Products

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