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-P2548
    pp60 (v-SRC) Autophosphorylation Site, Phosphorylated
    pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification.
    pp60 (v-SRC) Autophosphorylation Site, Phosphorylated
  • HY-144441
    NSC81111
    Inhibitor
    NSC81111 is a potent and orally active EGFR-TK inhibitor with an IC50 of 0.15 nM. NSC81111 has anticaner effects.
    NSC81111
  • HY-164503
    Neptinib
    Inhibitor
    Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFRwt, EGFRL858R/T790M, EGFRL858R and EGFRT790M, respectively.
    Neptinib
  • HY-N14638
    Paeciloquinone D
    Inhibitor
    Paeciloquinone D can inhibit the EGFR protein tyrosine kinase.
    Paeciloquinone D
  • HY-169948
    BML-265
    Inhibitor
    BML-265 is a potent EGFR tyrosine kinase inhibitor. BML-265 disrupts Golgi integrity and abolishes secretory protein transport of diverse cargos. BML-265 affects Golgi integrity and transport in human cells but not in rodent cells.
    BML-265
  • HY-15769A
    WHI-P180 hydrochloride
    Inhibitor
    WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
    WHI-P180 hydrochloride
  • HY-169755
    Tyrphostin 63
    Inhibitor
    Tyrphostin 63 (compound 13) is an epidermal growth factor receptor (EGFR) inhibitor with IC50 and Ki values are 375 and 123 μM, respectively.
    Tyrphostin 63
  • HY-156991
    NODAGA-NHS
    NODAGA-NHS (NODA-GA-NHS ester) is a [64]Cu chelator and the dissociated form of DOTA-trastuzumab in vivo. NODAGA-NHS was added in 0.1 M borate buffer at a ratio of 5/20/100 and was able to effectively bind trastuzumab (10 mg/mL) (4°C, 20 h). The copper content of the [64]Cu-NODAGA-trastuzumab was up to 80%. After blood was drawn from the caudal vein of mice, [64]Cu-NODAGA-trastuzumab was injected and showed good tumor uptake in mice expressing HER2 tumors, showing good PET imaging tracking ability.
    NODAGA-NHS
  • HY-50898R
    Lapatinib (Standard)
    Inhibitor
    Lapatinib (Standard) is the analytical standard of Lapatinib. This product is intended for research and analytical applications. 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.
    Lapatinib (Standard)
  • HY-50898CS
    Lapatinib-d4 tosylate
    Inhibitor
    Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active 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-d<sub>4</sub> tosylate
  • HY-169570
    EGFR-IN-149
    Inhibitor
    EGFR-IN-149 (Compound 3-OH) is an EGFR inhibitor (IC50: 0.42 nM).
    EGFR-IN-149
  • HY-P10648
    Herceptide
    Herceptide (HER2-targeting peptide) is a HER2-targeting peptide, and can be further conjugated to the near-infrared fluorescent dye indocyanine green (HY-D0711) (ICG) for developing theranostic agents.
    Herceptide
  • HY-163396
    EGFR-IN-107
    Inhibitor
    EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFRWT and 0.0438 μM for EGFRL858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research.
    EGFR-IN-107
  • HY-169566
    EGFR-IN-146
    Inhibitor
    EGFR-IN-146 is an EGFR inhibitor that can inhibit the EGFR signaling pathway and improve insulin sensitivity by activating the AMPK pathway, which can effectively reduce blood sugar levels and body weight. EGFR-IN-146 has great potential in the study of diabetes and obesity.
    EGFR-IN-146
  • HY-157582
    MS39N
    Control
    MS39N (compound 27) is a negative control for MS39 that binds EGFR without inducing degradation.
    MS39N
  • 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) is the analytical standard of Tyrphostin 25. This product is intended for research and analytical applications. Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase. Tyrphostin 25 is also a GPR35 agonist with an IC50 of 0.94 µM and 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-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[1][2].
    Gefitinib-d<sub>3</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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