1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

EGFR

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 Related Products (428):

Cat. No. Product Name Effect Purity
  • HY-P9905
    Cetuximab Inhibitor 99.70%
    Cetuximab (C225) is a human IgG1 monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for EGFR by SPR. Cetuximab has potent antitumor activity[1].
  • HY-10261
    Afatinib Inhibitor 99.93%
    Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer[1][2][3][4].
  • HY-P9907
    Trastuzumab Inhibitor 99.80%
    Trastuzumab is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
  • HY-15772
    Osimertinib Inhibitor 99.92%
    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
  • HY-50896
    Erlotinib Inhibitor 99.99%
    Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer[1].
  • HY-P99969
    Inetetamab Inhibitor
    Inetetamab is a monoclonal antibody binding to domain IV of HER2 receptor. Inetetamab alone or together with tyrosine kinase inhibitors has antitumor activities[1][2].
  • HY-103439
    GW583340 dihydrochloride Inhibitor
    GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50: 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride reverses ABCG2- and ABCB1-mediated drug resistance. GW 583340 dihydrochloride has anti-cancer activity[1][2][3].
  • HY-149275
    PKM2/PDK1-IN-1 Inhibitor
    PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway[1].
  • HY-132883
    EGFR/CSC-IN-1 Inhibitor
    EGFR/CSC-IN-1 is a potential EGFR (IC50 10.52 nM) and cancer stem cell (CSC) dual inhibitor for triple-negative breast cancer research.
  • HY-10261S
    Afatinib D6 Inhibitor
    Afatinib-d6 is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor[1].
  • HY-129550
    BI-4020 Inhibitor
    BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties[1].
  • HY-143733
    HER2-IN-5 Inhibitor
    HER2-IN-5 is a potent and orally active HER-2 inhibitor, example 10, extracted from patent WO2021164697[1].
  • HY-10251
    BMS-599626 Inhibitor
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy[1][2].
  • HY-147413
    Unecritinib Inhibitor
    Unecritinib (TQ-B3101) is a potent EGFR tyrosine kinase inhibitor. Unecritinib shows anticancer activity. Unecritinib inhibits ALK, ROS1, and MET. Unecritinib has the potential for the research of solid tumor and relapsed or refractory ALK-positive anaplastic large cell lymphoma[1][2].
  • HY-144053
    EGFR-IN-36 Inhibitor
    EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research[1].
  • HY-131066
    EMI48 Inhibitor 99.02%
    EMI48, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI48 inhibits EGFR triple mutants[1].
  • 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[1][2].
  • HY-147941
    MS9427 Degrader
    MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer[1].
  • HY-50898S3
    Lapatinib-d4-1 Inhibitor
    Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) 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].
  • HY-147802
    EGFR-IN-59 Inhibitor
    EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC50=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer[1].