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-13595
    Chrysophanol
    		Inhibitor 99.77%
    Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
    Chrysophanol
  • HY-N0281
    Daphnetin
    		Inhibitor 99.86%
    Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.
    Daphnetin
  • HY-32718
    Pelitinib
    		Inhibitor 98.80%
    Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
    Pelitinib
  • HY-10261A
    Afatinib dimaleate
    		Inhibitor 99.88%
    Afatinib (BIBW 2992) dimaleate 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 dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib dimaleate
  • HY-100848
    TX1-85-1
    		Inhibitor 98.04%
    TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
    TX1-85-1
  • HY-19730
    Olmutinib
    		Inhibitor 99.88%
    Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC.
    Olmutinib
  • HY-18957
    Lifirafenib
    		Inhibitor 98.73%
    Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
    Lifirafenib
  • HY-16558
    Butein
    		Inhibitor 99.95%
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
    Butein
  • HY-14346
    PD153035
    		Inhibitor 98.83%
    PD153035 (SU-5271; AG1517; ZM 252868) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.
    PD153035
  • HY-15729
    Rociletinib
    		Inhibitor 99.79%
    Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
    Rociletinib
  • HY-P9907A
    Trastuzumab (anti-HER2)
    		Inhibitor 99.62%
    Trastuzumab (PBS) is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab (PBS) has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
    Trastuzumab (anti-HER2)
  • HY-N0280
    Corosolic acid
    		99.23%
    Corosolic acid (Colosolic acid) isolated from the fruit of Cratoegus pinnatifida var. psilosa, was reported to have anticancer activity. Corosolic acid induces cancer cell apoptosis.
    Corosolic acid
  • HY-123921
    Gefitinib-based PROTAC 3
    		Inhibitor 99.98%
    Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.
    Gefitinib-based PROTAC 3
  • HY-N2409
    Delphinidin chloride
    		Inhibitor ≥98.0%
    Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC50: 1.3 μM), shutting down downstream signaling cascades.
    Delphinidin chloride
  • HY-18750
    Zorifertinib
    		Inhibitor 99.76%
    Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFRwt, EGFRL858R, and EGFRexon 19Del, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research.
    Zorifertinib
  • HY-50898A
    Lapatinib ditosylate
    		Inhibitor 99.98%
    Lapatinib ditosylate (GW572016 ditosylate) 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.
    Lapatinib ditosylate
  • HY-100213
    EAI045
    		Inhibitor 99.08%
    EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.
    EAI045
  • HY-P9968
    Nimotuzumab
    		Inhibitor
    Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a KD of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC).
    Nimotuzumab
  • HY-13314
    Tesevatinib
    		Inhibitor 99.21%
    Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, VEGFR2/KDR/Flk-1, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.
    Tesevatinib
  • HY-79077
    Osimertinib dimesylate
    		Inhibitor 99.96%
    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
    Osimertinib dimesylate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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