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-P991508
    Sym004
    Inhibitor
    Sym004 is a 1:1 mixture of two recombinant, human-mouse chimeric mAbs directed against nonoverlapping EGFR epitopes (mAb992 and mAb1024). Sym004 is ability to mediate rapid EGFR internalization and subsequent degradation of internalized receptors via EGFR cross-linking. Sym004 can be used for the study of metastatic colorectal cancer, head and neck (H&N) and lung cancer.
    Sym004
  • HY-50898BR
    Lapatinib ditosylate monohydrate (Standard)
    Inhibitor
    Lapatinib (ditosylate monohydrate) (Standard) is the analytical standard of Lapatinib (ditosylate monohydrate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-158828
    SSO111 sodium
    SSO111 sodium, a 20mer fully modified antisense oligonucleotide, targets the oncogene?HER2. SSO111 sodium induces exon 15 skipping during splicing, leading to the generation of a novel mRNA transcript that excludes exon 15. SSO111 sodium downregulated HER2 mRNA, which resulted in the inhibition of proliferation and induction of apoptosis in HER2-overexpressing tumor cells.
    SSO111 sodium
  • HY-101958R
    Tyrphostin 25 (Standard)
    Inhibitor
    Tyrphostin 25 (Standard) (AG82 (Standard)) is the analytical standard of Tyrphostin 25 (HY-101958). This product is intended for research and analytical applications. Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase with an IC50 value of 3 µM in A431 cells. Tyrphostin 25 is also a GPR35 agonist with an EC50 of 5.3 µM.
    Tyrphostin 25 (Standard)
  • HY-117523
    (Z)-RG-13022
    Inhibitor
    (Z)-RG-13022 is a tyrosine kinase (TK) inhibitor, which inhibits preferentially the TK activity of the EGF receptor and inhibits EGF-stimulated growth of cultured cells. (Z)-RG-13022 exerts an IC50 of 11 μM for DNA synthesis in the HN5 cells, which is 3 times more potent than (E)-RG-13022 (IC50=38 μM). (Z)-RG-13022 can be used for research of breast cancer cells.
    (Z)-RG-13022
  • HY-13524R
    AG-1478 (Standard)
    Inhibitor
    AG-1478 (Standard) is the analytical standard of AG-1478. This product is intended for research and analytical applications. AG-1478 (Tyrphostin AG-1478) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 has antiviral effects against HCV and encephalomyocarditis virus (EMCV).
    AG-1478 (Standard)
  • HY-101006R
    Methyl 2,5-dihydroxycinnamate (Standard)
    Inhibitor
    Methyl 2,5-dihydroxycinnamate (Standard) is the analytical standard of Methyl 2,5-dihydroxycinnamate. This product is intended for research and analytical applications. Methyl 2,5-dihydroxycinnamate is an erbstatin analog and a stable, potent inhibitor of EGFR kinase activity.
    Methyl 2,5-dihydroxycinnamate (Standard)
  • HY-50895S2
    Gefitinib-d3
    Inhibitor
    Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
    Gefitinib-d<sub>3</sub>
  • HY-129510R
    4-Methyl erlotinib (Standard)
    Inhibitor
    4-Methyl erlotinib (Standard) is the analytical standard of 4-Methyl erlotinib. This product is intended for research and analytical applications. 4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers.
    4-Methyl erlotinib (Standard)
  • HY-N14639
    Paeciloquinone E
    Inhibitor
    Paeciloquinone E can inhibit the EGFR protein tyrosine kinase.
    Paeciloquinone E
  • HY-135815AR
    Mobocertinib succinate (Standard)
    Inhibitor
    Mobocertinib (succinate) (Standard) is the analytical standard of Mobocertinib (succinate). This product is intended for research and analytical applications. Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research.
    Mobocertinib succinate (Standard)
  • HY-P990698
    Umizortamig
    Umizortamig is an anti-CD3E/EGFR/TNFRSF9/PD-L1/CD3G monoclonal antibody.
    Umizortamig
  • HY-32718S
    Pelitinib-d6
    Pelitinib-d6 (EKB-569-d6) is the deuterium labeled Pelitinib. Pelitinib (EKB-569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
    Pelitinib-d6
  • HY-164919
    Calotatug ginistinag
    Inhibitor
    Calotatug ginistinag (XMT-2056) is an antibody-drug conjugate targeting HER2, with an effective payload connected via a linker (LP, HY-148067) to a STING agonist (STING agonist-20, HY-148068), and has potential immune activation and anticancer activity.
    Calotatug ginistinag
  • HY-168305
    EGFR ligand-11
    EGFR ligand-11 is a target protein ligand for EGFR and can be used to synthesize PROTAC MS154 (HY-141640).
    EGFR ligand-11
  • HY-19909A
    NRC-2694-A
    Inhibitor
    NRC-2694-A is an orally effective EGFR tyrosine kinase inhibitor. NRC-2694-A can be used in the study of malignant squamous cell carcinoma (HNSCC).
    NRC-2694-A
  • HY-16069AR
    Tucatinib hemiethanolate (Standard)
    Inhibitor
    Tucatinib (hemiethanolate) (Standard) is the analytical standard of Tucatinib (hemiethanolate). This product is intended for research and analytical applications. Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
    Tucatinib hemiethanolate (Standard)
  • HY-135727
    PF-6422899
    Inhibitor
    PF-6422899 is an inhibitor for EGFR, that it selectively binds to EGFR and SOAT1 in nanomolar levels.
    PF-6422899
  • HY-P991092
    IBI-334
    Inhibitor
    IBI-334 is a bispecific B7-H3 and EGFR antibody. IBI-334 has an EGFR arm for signal blockage and is coupled with a fine-tuned B7-H3 arm with optimal affinity and binding domain. IBI-334 is afucosylated to enhance its antibody-mediated cell cytotoxicity (ADCC) effects. IBI-334 has a wide range of applications in many EGFR-driven solid tumors.
    IBI-334
  • HY-100064R
    O-Desmethyl gefitinib (Standard)
    Inhibitor
    O-Desmethyl gefitinib (Standard) is the analytical standard of O-Desmethyl gefitinib. This product is intended for research and analytical applications. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays.
    O-Desmethyl gefitinib (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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