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-147942
    MS9449
    98.95%
    MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer.
    MS9449
  • 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-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-143319
    SPH5030
    Inhibitor 99.40%
    SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2WT and EGFRWT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer.
    SPH5030
  • 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 99.40%
    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-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-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-112345
    PD-089828
    Inhibitor 98.07%
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
    PD-089828
  • 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
  • HY-P1828A
    EGFRvIII peptide (PEPvIII) TFA
    98.73%
    EGFRvIII peptide (PEPvIII) TFA is a tumor-specific mutation that is widely expressed in glioblastoma multiforme (GBM) and other neoplasms and its expression enhances tumorigenicity. EGFRvIII peptide TFA represents a truly tumor-specific target for antitumor immunotherapy.
    EGFRvIII peptide (PEPvIII) TFA
  • HY-P99306
    Modotuximab
    Inhibitor 99.08%
    Modotuximab (DS 1024) is an IgG1κ-type chimeric antibody targeting human EGFR protein. Modotuximab binds non-overlapping epitopes on domain III of EGFR, a domain that is intact in EGFRvIII. Modotuximab has antitumor activity in vivo.
    Modotuximab
  • HY-157480
    EGFR/AURKB-IN-1
    Inhibitor 99.43%
    EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of L858R EGFR and AURKB with IC50s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research.
    EGFR/AURKB-IN-1
  • HY-13984
    Mutant EGFR inhibitor
    Inhibitor 99.51%
    Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M.
    Mutant EGFR inhibitor
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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