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-164490
    LS-106
    Inhibitor
    LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model.
    LS-106
  • HY-E70707
    EGFR L858R Recombinant Human Active Protein Kinase
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L858R Recombinant Human Active Protein Kinase is a recombinant EGFR L858R protein that can be used to study EGFR L858R-related functions.
    EGFR L858R Recombinant Human Active Protein Kinase
  • HY-163419
    HER2-IN-18
    Inhibitor
    HER2-IN-18 is a HER2 inhibitor, with an IC50 less than 200 nM for HER-YVMA and HER-WT. HER2-IN-18 can be used for cancer research.
    HER2-IN-18
  • HY-162099
    VEGFR-IN-4
    Inhibitor
    VEGFR-IN-4 (Compound 6e) is an epidermal growth factor receptor (EGFR) inhibitor. VEGFR-IN-4 has potent antiproliferative activity with an IC50 value of 24.6nM against HCC827 cells.
    VEGFR-IN-4
  • 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-146210
    EGFR-IN-50
    Inhibitor
    EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells.
    EGFR-IN-50
  • HY-N1988R
    Cucurbitacin IIa (Standard)
    Inhibitor
    Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC50 of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.
    Cucurbitacin IIa (Standard)
  • HY-142283BS
    N-Desmethyl dosimertinib-d5
    N-Desmethyl dosimertinib-d5 is the deuterium labeled N-Desmethyl dosimertinib.
    N-Desmethyl dosimertinib-d<sub>5</sub>
  • HY-144444
    NSC381467
    Inhibitor
    NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases.
    NSC381467
  • HY-146228
    HSP90-IN-13
    Inhibitor
    HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway.
    HSP90-IN-13
  • HY-RS04473
    Erbb4 Mouse Pre-designed siRNA Set A
    Inhibitor

    Erbb4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Erbb4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Erbb4 Mouse Pre-designed siRNA Set A
  • HY-138627AR
    AST5902 trimesylate (Standard)
    Inhibitor
    AST5902 (trimesylate) (Standard) is the analytical standard of AST5902 (trimesylate). This product is intended for research and analytical applications. AST5902 trimesylate is the principal metabolite of Alflutinib (AST2818) both in vitro and in vivo. AST5902 trimesylate exerts antineoplastic activity. Alflutinib is an EGFR inhibitor[1].
    AST5902  trimesylate (Standard)
  • HY-114535
    Jaceidin
    Inhibitor
    Jaceidin is a promising lead molecule for potent VEGFR inhibitor with excellent membrane permeability and oral bioavailability. Jaceidin exhibits anti-tumor activities.
    Jaceidin
  • HY-10188
    SKS-927
    Inhibitor
    SKS-927 is a Src kinase inhibitor, with an IC50 value of 3.9 nM. SKS-927 inhibits the proliferation of Src-transformed rat fibroblasta, with an IC50 value of 73 nM. SKS-927 exhibits an IC50 value of 720 nM against EGFR. SKS-927 can be used for the study of cancer and osteoporosis.
    SKS-927
  • HY-P10569
    Biotin HER-2 substrate peptide
    Biotin HER-2 substrate peptide is a substrate of Her4 and Her2/neu tyrosine kinase with a Km value of 60 μm for Her2/neu kinase domain.
    Biotin HER-2 substrate peptide
  • HY-178442
    EGFR-IN-179
    Inhibitor
    EGFR-IN-179 (Compound 8d) is an EGFR inhibitor (IC50: 0.068 μM for EGFR L858R/T790M/C797S; 2.56 μM for EGFR-WT-TK). EGFR-IN-179 has anticancer activity against non-small cell lung cancer.
    EGFR-IN-179
  • HY-143323
    HER2-IN-9
    Inhibitor
    HER2-IN-9 is an orally active HER2 inhibitor, with an IC50 value of 0.03 μM. HER2-IN-9 inhibits HER-2 positive breast cancer cells proliferation and migration. HER2-IN-9 can be used in the research of breast cancers.
    HER2-IN-9
  • HY-173367
    Anticancer agent 271
    Inhibitor
    Anticancer agent 271 (compound 5C) has antiproliferative activity against lung (A549), colon (Caco-2) cancer cell lines, and human lung fibroblast (WI38) with an IC50 value of 9.18 μM on A549 cells. Anticancer agent 271 downregulates PI3K and mTOR gene expression that can be used for cancer research.
    Anticancer agent 271
  • HY-175809
    SRT6
    Inhibitor
    SRT6 is a CD44 inhibitor. SRT6 exerts antiproliferative activity in CD44+ breast cancer and lung cancer cells. SRT6 inhibits CD44-associated SRC kinase, as well as EGFR, ERBB2, ERBB4, MAP3K10 and MAPKAPK2. SRT6 can be used for the research of breast cancer and lung cancer.
    SRT6
  • HY-149344
    Anticancer agent 133
    Inhibitor
    Anticancer agent 133 (compound Rh2) is an anti-cancer agent with cytotoxic and antimetastatic activities. Anticancer agent 133 induces cell cycle arrest, apoptosis, and autophagy. Anticancer agent 133 also inhibits cell metastasis via suppression of EGFR expression mediated by FAK-regulated integrin β1.
    Anticancer agent 133
Cat. No. Product Name / Synonyms Species Source
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