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-15772S
    Osimertinib-d6
    Inhibitor 99.70%
    Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
    Osimertinib-d<sub>6</sub>
  • HY-153110A
    Larotinib mesylate hydrate
    Inhibitor 98.66%
    Larotinib mesylate hydrate 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 mesylate hydrate
  • HY-150023
    BI-1622
    Inhibitor 98.97%
    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-P99216
    Ponezumab
    Inhibitor 99.39%
    Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease.
    Ponezumab
  • HY-P990071
    Fepixnebart
    Inhibitor
    Fepixnebart is a humanized IgG4κ antibody targeting TGF-alpha (TGFA).
    Fepixnebart
  • HY-150024
    BI-4142
    Inhibitor 98.39%
    BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM.
    BI-4142
  • HY-136430
    JCN037
    Inhibitor 99.76%
    JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.
    JCN037
  • 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-111415
    EGFR-IN-5
    Inhibitor 99.49%
    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.
    EGFR-IN-5
  • HY-17499
    EGFR-IN-12
    Inhibitor 99.60%
    EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFRL858R and EGFRL861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
    EGFR-IN-12
  • HY-108484
    PP 3
    Inhibitor 98.78%
    PP 3 (Compound 3) is an EGFR tyrosine kinase inhibitor with an IC50 of 2.7 μM.
    PP 3
  • HY-P10224A
    G7-18NATE TFA
    98.59%
    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-112420
    EGFR/ErbB-2/ErbB-4 inhibitor-2
    Inhibitor 99.45%
    EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM.
    EGFR/ErbB-2/ErbB-4 inhibitor-2
  • HY-15336
    AG 555
    Inhibitor ≥98.0%
    AG 555 (Tyrphostin AG 555), a potent antiretroviral agent, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation.
    AG 555
  • HY-50895R
    Gefitinib (Standard)
    Inhibitor
    Gefitinib (Standard) is the analytical standard of Gefitinib. This product is intended for research and analytical applications. 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 and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
    Gefitinib (Standard)
  • HY-161126
    EGFR-IN-98
    Inhibitor 99.12%
    EGFR-IN-98 (Compound 4c) is a EGFR inhibitor. The IC50 values of L858R/T790M/C797S and Del19/T790M/C797S are 0.277 μM and 0.089 μM, respectively. EGFR-IN 98 can be used in the study of tumors.
    EGFR-IN-98
  • HY-12008S
    Erlotinib-d6 hydrochloride
    Inhibitor 98.13%
    Erlotinib-d6 hydrochloride a deuterium labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib-d6 (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-d<sub>6</sub> hydrochloride
  • HY-103566
    LY456236
    Inhibitor 99.81%
    LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM.
    LY456236
  • HY-144304
    PROTAC EGFR degrader 2
    Inhibitor
    PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC.
    PROTAC EGFR degrader 2
  • HY-P99461
    Barecetamab
    Inhibitor
    Barecetamab (ISU-104) is a fully human anti-ErbB3 monoclonal antibody. Barecetamab can be used for the research of recurrent/metastatic (R/M) head and neck squamous cell carcinoma (HNSCC).
    Barecetamab
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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