2. Signaling Pathways
  3. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  4. EGFR

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

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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.

EGFR Isoform Specific Products:

EGFR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • 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-155736
    MAPK-IN-2
    		Inhibitor 98.54%
    MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFRT790M IC50=69 nM and B-RAFV600E IC50=83 nM).
    MAPK-IN-2
  • HY-135805B
    (Rac)-JBJ-04-125-02 acetate
    (Rac)-JBJ-04-125-02 acetate is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, selective mutagenesis, allosteric and orally active EGFR inhibitor.
    (Rac)-JBJ-04-125-02 acetate
  • HY-108016
    Peruvoside
    		Inhibitor 99.32%
    Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib.
    Peruvoside
  • HY-103442
    CGP52411
    		Inhibitor 99.82%
    CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
    CGP52411
  • HY-13897
    CNX-2006
    		Inhibitor 98.42%
    CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFRT790M.
    CNX-2006
  • 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-139300A
    Epitinib succinate
    		Inhibitor 99.01%
    Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer. Epitinib (succinate) 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 succinate
  • HY-132842A
    (S)-Sunvozertinib
    		Inhibitor 99.14%
    (S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
    (S)-Sunvozertinib
  • HY-153901
    PROTAC EGFR degrader 8
    		Inhibitor 98.90%
    PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader. PROTAC EGFR degrader 8 degrades EGFR in HCC827 cell with a DC50 of 15.56 nM. PROTAC EGFR degrader 8 inhibits H1975, PC-9, HCC827 cell growth with IC50s of 7.72 nM, 121.9 nM, 14.21 nM. PROTAC EGFR degrader 8 can be used for research of cancer, especially NSCLC.
    PROTAC EGFR degrader 8
  • HY-50898S
    Lapatinib-d4
    		Inhibitor 99.02%
    Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1][2].
    Lapatinib-d<sub>4</sub>
  • HY-W013857
    Lavendustin C
    		Inhibitor 98.32%
    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
  • 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-P1855
    HER2/neu (654-662) GP2
    		98.04%
    HER2/neu (654-662) GP2 is a nine amino acid peptide derived from the human epidermal growth factor receptor 2 (HER2/nue, 654–662), induces HLA-A2-restricted cytotoxic T lymphocytes (CTL) reactive to various epithelial cancers.
    HER2/neu (654-662) GP2
  • HY-161537
    EGFR ligand-9
    		Inhibitor 98.80%
    EGFR ligand-9 is an EGFR ligand. EGFR ligand-9 can be used for synthesis of PROTAC EGFR degrader 9 (HY-161536).
    EGFR ligand-9
  • HY-W018800
    4(3H)-Quinazolinone
    		Inhibitor 99.91%
    4(3H) -quinazolinone is a fused nitrogen heterocyclic compound whose derivatives have a wide range of antimicrobial and antitumor activities.
    4(3H)-Quinazolinone
  • 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-153111
    EGFR/HER2-IN-9
    		Inhibitor 98.73%
    EGFR/HER2-IN-9 (Compound 1) is an EGFR and HER2 inhibitor with IC50s of 3.2, 8.3 and 14 nM against EGFR, EGFR T790M and HER2, respectively.
    EGFR/HER2-IN-9
  • HY-118532
    Tyrphostin AG30
    		Inhibitor 99.70%
    Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
    Tyrphostin AG30
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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