1. シグナル伝達
  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.

製品番号 製品名 製品効果 純度 構造式
  • HY-N1988
    Cucurbitacin IIa

    Cucurbitacin IIa

    Inhibitor 99.90%
    Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable EGFR inhibitor with an IC50 of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the EGFR-MAPK signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer.
    Cucurbitacin IIa
  • HY-P2503
    EGFR Protein Tyrosine Kinase Substrate 99.46%
    EGFR Protein Tyrosine Kinase Substrate is a EGFR protein tyrosine kinase substrate.
    EGFR Protein Tyrosine Kinase Substrate
  • HY-10346
    AV-412 Inhibitor 99.17%
    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
    AV-412
  • HY-P99969
    Inetetamab Inhibitor
    Inetetamab is a monoclonal antibody binding to domain IV of HER2 receptor. Inetetamab alone or together with tyrosine kinase inhibitors has antitumor activities.
    Inetetamab
  • HY-175252
    PROTAC EGFR degrader 14 Degrader 99.26%
    PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFRC797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFRWT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)).
    PROTAC EGFR degrader 14
  • HY-P990755
    Pamvatamig
    Pamvatamig is an anti-EGFR/MET human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Pamvatamig
  • HY-161633
    PROTAC EGFR degrader 11 Degrader 99.20%
    PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a Ki of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <100 nM.
    PROTAC EGFR degrader 11
  • HY-12008R
    Erlotinib Hydrochloride (Standard) Inhibitor
    Erlotinib (Hydrochloride) (Standard) is the analytical standard of Erlotinib (Hydrochloride). This product is intended for research and analytical applications. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib (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.
    Erlotinib Hydrochloride (Standard)
  • HY-163428
    Perzebertinib Inhibitor
    ZN-A-1041 inhibits HER2 in BT474 cell and wt-EGFR in H838 cells, with IC50s of 9.5 nM and 12 μM respectively. ZN-A-1041 can be used for research of cancer and inflammation.
    Perzebertinib
  • HY-10251
    BMS-599626 Inhibitor 98.56%
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
    BMS-599626
  • HY-P99628
    Futuximab Inhibitor 98.09%
    Futuximab is a chimeric monoclonal antibody targeting non-overlapping epitopes on EGFR. Futuximab has antineoplastic activity.
    Futuximab
  • HY-150023
    BI-1622 Inhibitor 98.02%
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.
    BI-1622
  • HY-P99892
    Serclutamab 99.97%
    Serclutamab is a humanized chimeric antibody targeting EGFR IgG1-κ. Mainly expressed by CHO (Chinese Hamster Ovary) cells.
    Serclutamab
  • HY-12010
    BMS-599626 Hydrochloride Inhibitor 98.90%
    BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
    BMS-599626 Hydrochloride
  • HY-138627A
    AST5902 trimesylate Inhibitor 98.75%
    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.
    AST5902  trimesylate
  • HY-153110
    Larotinib Inhibitor 99.50%
    Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.
    Larotinib
  • HY-RS04209
    EGFR Human Pre-designed siRNA Set A Inhibitor

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

    EGFR Human Pre-designed siRNA Set A
  • HY-123035
    Gamendazole Inhibitor 99.44%
    Gamendazole, an indazole carboxylic acid (ICA), is an orally active, selective HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A) inhibitor. Gamendazole binds to the C-terminal nucleotide binding pocket of HSP90 and cause downregulation of clients AKT1 and ERBB2, but stabilizes the HSP90 heterocomplex. Gamendazole specifically inhibits the actin bundling function of EEF1A1, but does not bind to the nucleotide docking pocket nor inhibits the ribosome charging or protein translation functions of EEF1A1. Gamendazole, an antispermatogenic compound with antifertility effects, has the potential for reversible non-hormonal male contraceptive agent research.
    Gamendazole
  • HY-P10224A
    G7-18NATE TFA 98.06%
    G7-18NATE TFA is a peptide inhibitor of Grb7. G7-18NATE TFA binds to the Grb7-SH2 domain with micromolar affinity (Kd = 18.1 μM). G7-18NATE TFA inhibits cell proliferation, motility, cell invasion and 3D culture formation in several cancer cell lines.
    G7-18NATE TFA
  • HY-W013857
    Lavendustin C Inhibitor 98.17%
    Lavendustin C is a potent Ca2+ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC50 of 0.2 µM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC50=0.012 µM) and pp60c-src(+) kinase (IC50=0.5 µM) .
    Lavendustin C
製品番号 製品名 / Synonyms Species Source
製品番号 製品名 / Synonyms Application Reactivity

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