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-P99605
    Cinrebafusp alfa
    Inhibitor 98.53%
    Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research.
    Cinrebafusp alfa
  • HY-141481
    DP-C-4
    Inhibitor 98.15%
    DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP.
    DP-C-4
  • HY-153110
    Larotinib
    Inhibitor 99.50%
    Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.
    Larotinib
  • HY-50898S
    Lapatinib-d4
    Inhibitor 99.02%
    Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib 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-d<sub>4</sub>
  • HY-W013857
    Lavendustin C
    Inhibitor 98.32%
    Lavendustin C is a potent Ca2+ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC50 of 0.2 µM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC50=0.012 µM) and pp60c-src(+) kinase (IC50=0.5 µM) .
    Lavendustin C
  • HY-N6577
    Astragaloside VI
    99.95%
    Astragaloside VI could activate EGFR/ERK signalling pathway to improve wound healing.
    Astragaloside VI
  • HY-P99685
    Laprituximab emtansine
    Inhibitor
    Laprituximab emtansine (IMGN-289) is an immunotoxin targeting HER1. Laprituximab emtansine is an EGFR antibody-drug conjugate (ADC) consisting of the J2898A antibody, DM1 (anti-microtubule agent) and the SMCC thioether linker. Laprituximab emtansine can be used for cancer research.
    Laprituximab emtansine
  • HY-15729A
    Rociletinib hydrobromide
    Inhibitor 98.04%
    Rociletinib hydrobromide (CO-1686 hydrobromide) 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 hydrobromide
  • HY-101429
    RG13022
    Inhibitor
    RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
    RG13022
  • HY-143337
    EGFR-IN-47
    Inhibitor
    EGFR-IN-47 is a potent and orally active EGFRL858R/T790M/C797S inhibitor with an IC50 of 0.01 μM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC.
    EGFR-IN-47
  • HY-100499
    Tyrphostin AG 528
    Inhibitor ≥98.0%
    Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with IC50s of 4.9 and 2.1 μM, respectively. Tyrphostin AG 528 (Tyrphostin B66) is a protein tyrosine kinase inhibitor, with IC50s of 4.9 μM for epidermal growth factor receptors (EGFR) and 2.1 μM for ErbB2. Tyrphostin AG 528 is also an anticancer agent.
    Tyrphostin AG 528
  • HY-171265
    MRG003
    Degrader
    MRG003 is an Antibody-Drug Conjugate (ADC) that consists of an anti-EGFR humanized IgG1 monoclonal antibody Becotatug (HY-P990049) and MMAE (HY-15162). These two parts are connected through a valine-citrulline (valine-citrulline) linker, where the linker and MMAE constitute the ADC's Drug-Linker conjugate VcMMAE (HY-15575).
    MRG003
  • HY-151159
    DHFR-IN-4
    Inhibitor 99.19%
    DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells.
    DHFR-IN-4
  • HY-156284
    EGFR-IN-89
    Inhibitor 98.75%
    EGFR-IN-89 (compound 13k) is a potent, fourth-generation EGFR mutation inhibitor with an IC50 of 10.1 nM against Del19/T790M/C797S mutations. EGFR-IN-89 shows higher selectivity over wild type.
    EGFR-IN-89
  • HY-10531
    ARRY-380 analog
    Inhibitor 99.19%
    ARRY-380 analog, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2.
    ARRY-380 analog
  • HY-161537
    EGFR ligand-9
    Inhibitor 98.80%
    EGFR ligand-9 is an EGFR ligand. EGFR ligand-9 can be used for synthesis of PROTAC EGFR degrader 9 (HY-161536).
    EGFR ligand-9
  • HY-149889
    EGFR-IN-78
    Inhibitor 99.57%
    EGFR-IN-78 (compound A5),a 2-aminopyrimidine derivative,is a reversible inhibitor of EGFRC797S-TK,and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity,inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase.
    EGFR-IN-78
  • HY-RS04472
    ERBB4 Human Pre-designed siRNA Set A
    Inhibitor

    ERBB4 Human Pre-designed siRNA Set A contains three designed siRNAs for ERBB4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    ERBB4 Human Pre-designed siRNA Set A
    ERBB4 Human Pre-designed siRNA Set A
  • HY-161927
    EGFR-TK-IN-4
    Inhibitor 99.90%
    EGFR-TK-IN-4 (compound 10k) is a potent and selective EGFR-TK inhibitor. EGFR-TK-IN-4 can induce apoptosis . EGFR-TK-IN-4 has antitumor activity.
    EGFR-TK-IN-4
  • HY-161408
    GePhos1
    GePhos1, a EGFR-targeting PhosTAC (phosphorylation targeting chimera), induces EGFR dephosphorylation. GePhos1 induces apoptosis.
    GePhos1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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