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-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-P991662
    AMG-595 Antibody
    AMG-595 Antibody is a EGFRvIII targeting antibody. AMG-595 Antibody can be used for synthesis of ADC AMG-595.
    AMG-595 Antibody
  • 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-E70706
    EGFR L718Q Recombinant Human Active Protein Kinase
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L718Q Recombinant Human Active Protein Kinase is a recombinant EGFR L718Q protein that can be used to study EGFR L718Q-related functions.
    EGFR L718Q Recombinant Human Active Protein Kinase
  • 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
  • HY-P990695
    Lunaxafusp
    		Inhibitor
    Lunaxafusp is an anti-ERBB2 scFv-heavy-κ monoclonal antibody composed of a single chain variable fragment, an antibody heavy chain, and a kappa antibody light chain.
    Lunaxafusp
  • HY-P10793
    Cyclic(YCDGFYACYMDV)
    		Inhibitor
    Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model.
    Cyclic(YCDGFYACYMDV)
  • HY-157402
    Topoisomerase II/EGFR-IN-1
    Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer.
    Topoisomerase II/EGFR-IN-1
  • HY-175608
    EGFR-IN-171
    		Inhibitor
    EGFR-IN-171 is an EGFR inhibitor with an IC50 value of 0.19 μM. EGFR-IN-171 also inhibits vascular endothelial growth factor 2 (VEGFR-2) with an IC50 value of 31.65 μM. EGFR-IN-171 can induce apoptosis and G2/M phase cell cycle arrest. EGFR-IN-171 can be used for cancer research, such as liver and breast cancer.
    EGFR-IN-171
  • HY-168968S
    ZJY-54
    		Inhibitor
    ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity.
    ZJY-54
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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