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-175009
    MRC-G-001
    Inhibitor
    MRC-G-001 is a Genipin (HY-17389) derivative with an IC50 of 117 μM against A549 cancer cells. MRC-G-001 inhibits the phosphorylation of EGFR, JAK1, and STAT3, and modulates epithelial-mesenchymal transition (EMT)-related protein expression, thereby attenuating cell migration and invasion. MRC-G-001 induces cell cycle arrest and cell apoptosis. MRC-G-001 can be used for the study of cancers such as non-small-cell lung cancer.
    MRC-G-001
  • HY-147860
    EGFR-IN-61
    Inhibitor
    EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively.
    EGFR-IN-61
  • HY-13524A
    AG-1478 hydrochloride
    Inhibitor
    AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV).
    AG-1478 hydrochloride
  • HY-RS04470
    Erbb3 Mouse Pre-designed siRNA Set A
    Inhibitor

    Erbb3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Erbb3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Erbb3 Mouse Pre-designed siRNA Set A
  • HY-19730A
    Olmutinib hydrochloride
    Inhibitor
    Olmutinib hydrochloride is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib hydrochloride is used for NSCLC.
    Olmutinib hydrochloride
  • HY-173164
    EGFR/BRAFV600E-IN-4
    Inhibitor
    EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAFV600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity.
    EGFR/BRAFV600E-IN-4
  • HY-159512
    EGFR kinase inhibitor 7
    Inhibitor
    EGFR kinase inhibitor 7 (compound 18i) is an EGFR inhibitor (IC50=42.3 nM) with anticancer activity. EGFR kinase inhibitor 7 has significant in vitro cytotoxicity and apoptosis induction ability. EGFR kinase inhibitor 7 has antiproliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values ​​of 4.82 µM and 1.43 µM, respectively.
    EGFR kinase inhibitor 7
  • HY-175316
    EGFR-IN-168
    Inhibitor
    EGFR-IN-168 (Compound 9a) is a potent EGFR inhibitor with an IC50 of 0.069 μM. EGFR-IN-168 has antitumor activity.
    EGFR-IN-168
  • HY-161603
    EGFR/HER2-IN-14
    Inhibitor
    EGFR/HER2-IN-14 (Compd 46) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research.
    EGFR/HER2-IN-14
  • HY-P10792
    HER2-targeted peptide H6F
    HER2-targeted peptide H6F is a HER2 targeting peptide that binds to HER2 to target breast cancer cells, with the amino acid sequence YLFFVFER. The HER2-targeted peptide H6F can be conjugated with the bifunctional chelating agent hydrazinonicotinamide (HYNIC) for radiolabeling with 99mTc. Single-photon emission computed tomography (SPECT) imaging shows that the labeled HER2-targeted peptide H6F specifically accumulates in HER2-positive MDA-MBA-453 tumor-bearing mice models. The HER2-targeted peptide H6F can be used for tumor molecular imaging studies.
    HER2-targeted peptide H6F
  • HY-10368
    EGFR/VEGFR2-IN-4
    Inhibitor
    EGFR/VEGFR2-IN-4 (Compound 19) is the irreversible inhibitor for EGFR and VEGFR-2 with IC50 of 18.7 nM and 102.3 nM, under the presence of 1 μM ATP.
    EGFR/VEGFR2-IN-4
  • HY-P990408
    Anti-ERBB1/EGFR/HER1 Antibody
    Inhibitor
    The Anti-ERBB1/EGFR/HER1 Antibody is a CHO-expressed human antibody that targets ERBB1/EGFR/HER1. The Anti-ERBB1/EGFR/HER1 Antibody consists of a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for the Anti-ERBB1/EGFR/HER1 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-ERBB1/EGFR/HER1 Antibody
  • HY-175252
    PROTAC EGFR degrader 14
    Degrader
    PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFRC797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFRWT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)).
    PROTAC EGFR degrader 14
  • HY-P1085
    Epidermal Growth Factor Receptor Peptide (985-996)
    Chemical
    Epidermal Growth Factor Receptor Peptide (985-996) is an amino acid peptide fragment derived from positions 985-996 in epidermal growth factor receptor (EGFR).
    Epidermal Growth Factor Receptor Peptide (985-996)
  • HY-169308
    EGFR-IN-132
    Inhibitor
    EGFR-IN-132 (Compound 23) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 1.6, 0.025, 0.019, 0.022, and 0.029 nM. EGFR-IN-132 exhibits good pharmacokinetics characteristics with high oral exposure.
    EGFR-IN-132
  • HY-P991588
    HLX-22
    Antagonist
    HLX-22 is a humanized monoclonal antibody targeting HER2. HLX-22 induces apoptosis in HER2-overexpressing breast and gastric cancer cells combined with Trastuzumab (HY-P9907). HLX-22 has potent antitumor activity against advanced solid tumors.
    HLX-22
  • HY-170559
    EGFR-IN-141
    Inhibitor
    EGFR-IN-141 (Compound 8I) is the inhibitor for EGFR with an IC50 of 2.67 nM. EGFR-IN-141 exhibits cytotoxicity in cancer cell A549 with an IC50 of 13.75 μM. EGFR-IN-141 induces apoptosis and mitochondrial membrane depolarization, and exhibits potential antitumor efficacy.
    EGFR-IN-141
  • HY-156116
    EGFR/CDK2-IN-4
    Inhibitor
    EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC50s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 2.74 μM.
    EGFR/CDK2-IN-4
  • HY-151161
    EGFR/HER2-IN-8
    Inhibitor
    EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.
    EGFR/HER2-IN-8
  • HY-172820
    Trastuzumab envedotin
    Inhibitor
    Trastuzumab envedotin (DP303c) is a anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab envedotin is composed of the tubulin polymerization inhibitor Monomethyl auristatin E (MMAE) (HY-15162) to the anti-HER2 antibody DP001 via a cleavable linker. Trastuzumab envedotin can be used for the research of HER2-positive solid tumors, such as breast cancer, colorectal cancer, and gastric cancer.
    Trastuzumab envedotin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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