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-13450
    ZM 449829
    Inhibitor 99.73%
    ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3.
    ZM 449829
  • HY-P990913
    Dalmitamig
    HY-P990913 is an EGFR/CD28-targeting IgG4κ type human antibody, the recommed isotype control is Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).
    Dalmitamig
  • HY-107367
    Epertinib
    Inhibitor ≥98.0%
    Epertinib (S-22611) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib shows potent antitumor activity. Epertinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Epertinib
  • HY-50895S
    Gefitinib-d8
    Inhibitor 98.42%
    Gefitinib-d8 is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
    Gefitinib-d<sub>8</sub>
  • HY-145960
    MC-Val-Cit-PAB-Amide-TLR7 agonist 4
    Agonist 99.39%
    MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.
    MC-Val-Cit-PAB-Amide-TLR7 agonist 4
  • HY-135805A
    (Rac)-JBJ-04-125-02
    Inhibitor
    (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor.
    (Rac)-JBJ-04-125-02
  • HY-139300
    Epitinib
    Inhibitor
    Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer. Epitinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Epitinib
  • HY-100962
    (E)-AG 99
    Inhibitor 98.36%
    (E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
    (E)-AG 99
  • HY-119944
    JND3229
    Inhibitor 99.78%
    JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R/T790M/C797S, EGFRWT and EGFRL858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.
    JND3229
  • HY-19617A
    EGFR-IN-1 hydrochloride
    Inhibitor
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
    EGFR-IN-1 hydrochloride
  • HY-19617
    EGFR-IN-1
    Inhibitor
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
    EGFR-IN-1
  • HY-147941
    MS9427
    Degrader
    MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer.
    MS9427
  • HY-147183
    JBJ-09-063
    Inhibitor
    JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer.
    JBJ-09-063
  • HY-P99628
    Futuximab
    Inhibitor 98.09%
    Futuximab is a chimeric monoclonal antibody targeting non-overlapping epitopes on EGFR. Futuximab has antineoplastic activity.
    Futuximab
  • HY-130608
    Mutated EGFR-IN-3
    Inhibitor
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
    Mutated EGFR-IN-3
  • HY-138627
    AST5902
    Inhibitor
    AST5902 is the active metabolite of Firmonertinib (HY-112870) (EGFR inhibitor). AST5902 has antineoplastic activity.
    AST5902
  • HY-P99888
    Pimurutamab
    99.42%
    Pimurutamab is a humanized IgG1-κ antibody targeting EGFR. Mainly expressed by CHO-K1 cells.
    Pimurutamab
  • HY-P99831
    Coprelotamab
    99.74%
    Coprelotamab (GB-221) is an IgG-κ monoclonal antibody targeting EGFR2. The commonly used expression system for Coprelotamab is CHO DG44 (Chinese Hamster Ovary) cells.
    Coprelotamab
  • HY-147219
    SIAIS164018
    Inhibitor
    SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857).
    SIAIS164018
  • HY-128778
    Gozanertinib
    Inhibitor 98.37%
    Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy.
    Gozanertinib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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