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

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

Related Products

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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-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-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-164476
    ES-072
    		Inhibitor
    ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells.
    ES-072
  • 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)
  • HY-N14349
    Asterriquinone
    		Inhibitor
    Asterriquinone (ARQ), a Asterriquinone analog, is a Grb-2 binding inhibitor. Asterriquinone inhibits the Grb-2 binding activity to tyrosine phosphorylated EGFR, with an IC50 of 8.37 μM. Asterriquinone is a HIV1 reverse transcriptase inhibitor with a Ki of 2.3 μM. Asterriquinone also inhibits Grb-7 and PLC-γ binding activities..
    Asterriquinone
  • HY-104065BR
    Pyrotinib dimaleate (Standard)
    		Inhibitor
    Pyrotinib dimaleate (Standard) is the analytical standard of Pyrotinib dimaleate. This product is intended for research and analytical applications. Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
    Pyrotinib dimaleate (Standard)
  • HY-158829
    SSOe26 sodium
    SSOe26 sodium is a 15mer antisense oligonucleotide targeting?HER4. SSOe26 sodium induces exon 26 skipping, leading to the generation of a novel mRNA transcript that excludes exon 26 (CYT2 isoform). SSOe26 sodium decreases tumour growth in mouse xenografts.
    SSOe26 sodium
  • HY-164527
    Si306
    		Inhibitor
    Si306 is a Src inhibitor with antitumor activity. Si306 reduces the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), and inhibits the invasion of human glioblastoma (GBM).
    Si306
  • HY-10367AR
    Canertinib dihydrochloride (Standard)
    		Inhibitor
    Canertinib (dihydrochloride) (Standard) is the analytical standard of Canertinib (dihydrochloride). This product is intended for research and analytical applications. Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice.
    Canertinib dihydrochloride (Standard)
  • HY-103443A
    HKI-357 dimaleate
    		Inhibitor
    HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 dimaleate suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
    HKI-357 dimaleate
  • HY-10261BR
    (E/Z)-Afatinib (Standard)
    		Inhibitor
    (E/Z)-Afatinib (Standard) is the analytical standard of (E/Z)-Afatinib. This product is intended for research and analytical applications. (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.
    (E/Z)-Afatinib (Standard)
  • HY-N14640
    Paeciloquinone F
    		Inhibitor
    Paeciloquinone F can inhibit the EGFR protein tyrosine kinase.
    Paeciloquinone F
  • HY-P990947
    Tilatamig
    HY-P990947 is an EGFR/MET-targeting Ig(G1 -κ_G1 -λ2) type human antibody.
    Tilatamig
  • HY-32721S
    Neratinib-d6
    		Inhibitor
    Neratinib-d6 (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
    Neratinib-d<sub>6</sub>
  • HY-32721R
    Neratinib (Standard)
    		Inhibitor
    Neratinib (Standard) is the analytical standard of Neratinib. This product is intended for research and analytical applications. Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.
    Neratinib (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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