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

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

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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-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-175220
    4-TCPA
    		Inhibitor
    4-TCPA is a potent VEGFR2 inhibitor. 4-TCPA induces apoptosis and cell cycle arrest, likely through inhibition of VEGFR2 and EGFR signaling with additional effects on the mTOR pathway. 4-TCPA can inhibit the vitality and proliferation of various cancer cell lines. 4-TCPA can be used for the study of cancers such as lung cancer, breast cancer and leukemia.
    4-TCPA
  • 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-41404R
    Piperonylic acid (Standard)
    Piperonylic acid (Standard) is the analytical standard of Piperonylic acid. This product is intended for research and analytical applications. Piperonylic acid is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic Acid is a selective, mechanism-based inactivator of the trans-cinnamate 4-Hydroxylase. Piperonylic acid has anticancer, antioxidant and antibacterial activities.
    Piperonylic acid (Standard)
  • HY-13314R
    Tesevatinib (Standard)
    		Inhibitor
    Tesevatinib (Standard) is the analytical standard of Tesevatinib. This product is intended for research and analytical applications. 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 (Standard)
  • 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-15495B
    (3S)-Tanzisertib hydrochloride
    		Inhibitor
    (3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor (IC50 values for JNK1, JNK2, and JNK3 are 61, 7, and 6 nM, respectively). (3S)-Tanzisertib (hydrochloride) selectively inhibits ERK1, p38α, and EGFR (IC50 = 0.48, 3.4, and 0.38 μM, respectively). (3S)-Tanzisertib (hydrochloride) inhibits LPS-induced TNFα production in an acute rat PK-PD model. (3S)-Tanzisertib (hydrochloride) can be used in idiopathic pulmonary fibrosis (IPF) research.
    (3S)-Tanzisertib hydrochloride
  • 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-15164R
    Icotinib Hydrochloride (Standard)
    		Inhibitor
    Icotinib (Hydrochloride) (Standard) is the analytical standard of Icotinib (Hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-16069R
    Tucatinib (Standard)
    		Inhibitor
    Tucatinib (Standard) is the analytical standard of Tucatinib. This product is intended for research and analytical applications. Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
    Tucatinib (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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