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-168173
    EGFR-IN-130
    		Inhibitor
    EGFR-IN-130 (compound 14b) is an EGFR inhibitor and apoptosis inducer. EGFR-IN-130 triggers death of HeLa cancer cells via apoptosis induction..
    EGFR-IN-130
  • HY-144794
    EGFR-IN-46
    		Inhibitor
    EGFR-IN-46 is a potent EGFR and FAK dual inhibitor with IC50s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis.
    EGFR-IN-46
  • HY-163453
    HER2-IN-19
    		Inhibitor
    HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR with IC50 values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitory activity against tumor cells, IC50NCI-N87 = 1.63 nM, IC50BT474= 15.17 nM, IC50BaF3-HER2YVMA = 1.49 nM.
    HER2-IN-19
  • HY-12008S1
    Erlotinib-13C6 hydrochloride
    Erlotinib-13C6 hydrochloride is the 13C labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib-13C6 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-<sup>13</sup>C<sub>6</sub> hydrochloride
  • HY-P99155A
    Zalutumumab (powder)
    		Inhibitor
    Zalutumumab (powder) is a high affinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab (powder) binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab (powder) binds with IgG and its Fab fragment with EC50s of 7 and 19 nM, respectively. Zalutumumab (powder) can be used for the research of cancer.
    Zalutumumab (powder)
  • HY-W008914
    (E/Z)-CP-724714
    		Inhibitor
    (E/Z)-CP-724714 is a racemic compound of (E)-CP-724714 and (Z)-CP-724714 isomers. CP-724714 is a potent and selective orally active ErbB2 (HER2) inhibitor.
    (E/Z)-CP-724714
  • HY-131710
    PDE5-IN-3
    		Inhibitor
    PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity.
    PDE5-IN-3
  • HY-P991245
    Anti-ERBB3/HER3 (SGP1)
    		Inhibitor
    Anti-ERBB3/HER3 (SGP1) is a human monoclonal antibody (mAb) targeting ERBB3/HER3. Anti-ERBB3/HER3 (SGP1) inhibits Neuregulin stimulated growth of cultured breast cancer cells. Anti-ERBB3/HER3 (SGP1) can be used in breast cancer research.
    Anti-ERBB3/HER3 (SGP1)
  • HY-149518
    EGFR/BRAFV600E-IN-3
    		Inhibitor
    EGFR/BRAFV600E-IN-3 is a EGFR, BRAFV600E and EGFRT790M inhibitor with IC50 value of 57 nM, 68 nM and 9.70 nM. EGFR/BRAFV600E-IN-3 is an apoptotic inducer and also displays promising antioxidant activity.
    EGFR/BRAFV600E-IN-3
  • HY-157994
    EGFR WT/T790M-IN-2
    		Inhibitor
    EGFR WT/T790M-IN-2 (Compound 7c) is a EGFR T790M/WT inhibitor with IC50 values of 0.08 and 0.13 μM, respectively. EGFR WT/T790M-IN-2 induces apoptosis by blocking the G0-G1 phase (apoptosis). EGFR WT/T790M-IN-2 has antitumor activity.
    EGFR WT/T790M-IN-2
  • HY-168433
    LSD1/EGFR-IN-1
    		Inhibitor
    LSD1/EGFR-IN-1 (compound L-1) is a potent inhibitor of LSD1, EGFRT790M/L858R and EGFRL858R/T790M/C797S, with IC50s of 6.24 and 2.06 and 5.01 μM, respectively. LSD1/EGFR-IN-1 plays an important role in cancer research.
    LSD1/EGFR-IN-1
  • HY-112474
    Tyrphostin AG 112
    		Inhibitor 98.55%
    Tyrphostin AG 112 is an EGFR phosphorylation inhibitor.
    Tyrphostin AG 112
  • HY-147967
    EGFR-IN-63
    		Inhibitor
    EGFR-IN-63 is an EGFR inhibition (IC50: 0.096 μM) and it has anticancer activity in MCF-7 cells (IC50: 2.49 μM).
    EGFR-IN-63
  • HY-100663
    Gefitinib impurity 2
    		99.56%
    Gefitinib impurity 2 is the impurity of Gefitinib. Gefitinib (ZD1839; HY-50895) 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. Gefitinib has antitumour activity.
    Gefitinib impurity 2
  • HY-149517
    EGFR/BRAFV600E-IN-2
    		Inhibitor
    EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAFV600E, and EGFRT790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency.
    EGFR/BRAFV600E-IN-2
  • HY-157399
    EGFR/HER2-IN-10
    		Inhibitor
    EGFR/HER2-IN-10 (compound 9F) is a potent and selective dual EGFR/HER2 inhibitor with IC50s of 2.3 nM and 234 nM for EGFR and HER2, respectively. EGFR/HER2-IN-10 shows an effective antiproliferative action against prostate carcinoma.
    EGFR/HER2-IN-10
  • HY-169428
    EGFR-IN-138
    EGFR-IN-138 (compound 19) is a potent EGFR inhibitor，with IC50s of 37，2.6 and 1.9 nM for Wild-type，L858R and T790M EGFR，respectively.
    EGFR-IN-138
  • HY-168577
    KRAS G12D inhibitor 25
    		Degrader
    KRAS G12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 degrades ERBB2 with a DC50 of 0.1-1 μM.
    KRAS G12D inhibitor 25
  • HY-147826
    EGFR-IN-60
    		Inhibitor
    EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFRWT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio.
    EGFR-IN-60
  • HY-162890
    EGFR-IN-122
    		Inhibitor
    EGFR-IN-122 (compound Yfq07) is a potent EGFR inhibitor. EGFR-IN-122 suppresses the proliferation of PC-9GR and HCC827GR cells.
    EGFR-IN-122
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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