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-155005
    EGFR mutant-IN-2
    		Inhibitor
    EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFRL858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFRdel19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity.
    EGFR mutant-IN-2
  • HY-101007A
    (+)-Tyrphostin B44
    		Inhibitor
    (+)-Tyrphostin B44 (Tyrphostin AG 835) (Compound B50) is an EGRF inhibitor with antitumor activities.
    (+)-Tyrphostin B44
  • HY-12806
    AG1557
    		Inhibitor 99.54%
    AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194.
    AG1557
  • HY-12872B
    Nazartinib S-enantiomer
    		98.66%
    Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.
    Nazartinib S-enantiomer
  • HY-161618
    MJ04
    		Inhibitor 98.08%
    MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg).
    MJ04
  • HY-50895S1
    Gefitinib-d6
    		Inhibitor ≥98.0%
    Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) 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-d<sub>6</sub>
  • HY-155358
    Os30
    		Inhibitor 98.34%
    Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation.
    Os30
  • HY-108931
    AG 1406
    		Inhibitor 99.03%
    AG 1406 (compound M19) is a HER2 inhibitor, with an IC50 of 10.57 μM for HER2 in BT474 cell and >50 μM for EGFR in EGF-3T3 cell.
    AG 1406
  • HY-135805
    JBJ-04-125-02
    		Inhibitor
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
    JBJ-04-125-02
  • HY-158310
    SOS1/EGFR-IN-1
    		Inhibitor 99.54%
    SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM).
    SOS1/EGFR-IN-1
  • HY-144677
    pan-HER-IN-2
    		Inhibitor 98.10%
    pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFRT790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities.
    pan-HER-IN-2
  • HY-B0794A
    AZ7550 hydrochloride
    		Inhibitor 98.66%
    AZ7550 hydrochloride is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
    AZ7550 hydrochloride
  • HY-164763
    SHR-A1201
    		Inhibitor
    SHR-A1201 is a HER2-targeting antibody-drug conjugate (ADC). SHR-A1201 is composed of a humanized anti-HER2 antibody (HY-P9907), a linker SMCC (HY-42360), and a microtubulin inhibitor payload Mertansine (HY-19792). SHR-A1201 can be used for research in HER2-positive breast cancer.
    SHR-A1201
  • HY-13272S2
    Dacomitinib-d10 dihydrochloride
    		Inhibitor
    Dacomitinib-d10 dihydrochloride is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
    Dacomitinib-d<sub>10</sub> dihydrochloride
  • HY-164387
    Sutetinib
    		Inhibitor
    Sutetinib is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo.
    Sutetinib
  • HY-14347
    EBE-A22
    		Control 99.76%
    EBE-A22 is a derivative of PD153035, which can inhibit the phosphorylation of ErbB-1, but EBE-A22 does not have this activity.
    EBE-A22
  • HY-164718
    Sevabertinib
    		Inhibitor 99.90%
    Sevabertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with antitumor activity.
    Sevabertinib
  • HY-153111
    EGFR/HER2-IN-9
    		Inhibitor 98.73%
    EGFR/HER2-IN-9 (Compound 1) is an EGFR and HER2 inhibitor with IC50s of 3.2, 8.3 and 14 nM against EGFR, EGFR T790M and HER2, respectively.
    EGFR/HER2-IN-9
  • HY-111452
    EGFR-IN-85
    		Inhibitor
    EGFR-IN-85 (Compound 1) is an EGFR inhibitor. EGFR-IN-85 has IC50 value of 0.19 μM for EGFRvⅢ phosphorylation. EGFR-IN-85 can suppress EGFR signaling within tumors. EGFR-IN-85 can be used for Glioblastoma (GBM) research.
    EGFR-IN-85
  • HY-P2673
    Lys-Arg-Thr-Leu-Arg-Arg
    Lys-Arg-Thr-Leu-Arg-Arg (KRTLRR) is a hexapeptide. Lys-Arg-Thr-Leu-Arg-Arg is a substrate of protein kinase C from EGF receptor. Lys-Arg-Thr-Leu-Arg-Arg can be used to determine the activity of protein kinase C.
    Lys-Arg-Thr-Leu-Arg-Arg
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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