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-158018
    EGFR-TK-IN-2
    		Inhibitor
    EGFR-TK-IN-2 (compound 10b) is EGFR-TK inhibitor with the IC50 of 0.16 μM. EGFR-TK-IN-2 inhibits cell growth.
    EGFR-TK-IN-2
  • HY-147797
    EGFR/HER2/CDK9-IN-2
    		Inhibitor
    EGFR/HER2/CDK9-IN-2 (Compound 9) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 145.35, 129.07, and 117.13 nM, respectively. EGFR/HER2/CDK9-IN-2 exhibits remarkable antitumor activity.
    EGFR/HER2/CDK9-IN-2
  • 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.
    PKM2/PDK1-IN-1
  • HY-156097
    Anticancer agent 158
    		Inhibitor
    Anticancer agent 158 (compound 7c) is a potent anticancer agent. The IC50s for inhibiting HepG-2, MDA-MB-231, and HCT-116 cell lines are 7.93 μM, 9.28 μM, 13.28 μM, and 181.89 μM, respectively.
    Anticancer agent 158
  • HY-164489
    KU004
    		Inhibitor
    KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative.
    KU004
  • HY-158177
    EGFR T790M/L858R-IN-6
    		Inhibitor
    EGFR T790M/L858R-IN-6 (compound 53), a pyrimidine compound, is a potent EGFR T790M/L858R inhibitor. EGFR T790M/L858R-IN-6 shows 90.88% enzyme activity inhibition with 0.05 μM.
    EGFR T790M/L858R-IN-6
  • HY-50896S1
    Erlotinib-13C6
    		Inhibitor
    Erlotinib-13C6 is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1].
    Erlotinib-<sup>13</sup>C<sub>6</sub>
  • HY-106204
    Nelipepimut-S
    Nelipepimut-S is a peptide vaccine which targets HER2. Nelipepimut-S has immune activity against HER2 positive breast cancer.
    Nelipepimut-S
  • HY-168469
    EGFR-IN-148
    		Inhibitor
    EGFR-IN-148 (compound 8c) is a potent inhibitor of EGFR , with the IC50 of 0.161 μM. EGFR-IN-148 causes G1/S arrest and markedly enhances apoptosis in HepG2 cells.
    EGFR-IN-148
  • HY-150782
    UNC-CA359
    		Inhibitor
    UNC-CA359 is a potent epidermal growth factor receptor (EGFR) inhibitor, with an IC50 value of 18 nM. UNC-CA359 exhibits strong anti-tumor activity, can be used to Chordoma research. UNC-CA359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    UNC-CA359
  • HY-158016
    Antiproliferative agent-49
    		Inhibitor
    Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC50 of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC50 values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS.
    Antiproliferative agent-49
  • HY-100636A
    Gefitinib N-oxide hydrochloride
    		Inhibitor
    Gefitinib N-oxide hydrochloride is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
    Gefitinib N-oxide hydrochloride
  • HY-155074
    EGFR-IN-79
    		Inhibitor
    EGFR-IN-79 (compound 21) is an EGFR inhibior with antitumor activity. EGFR-IN-79 induces ROS-independent apoptosis and EGFR/AKT/mTOR-mediated autophagy. EGFR-IN-79 induces cell death at both proliferating and quiescent zones of EJ28 spheroids. EGFR-IN-79 exhibits safety profile in the zebrafish-based model.
    EGFR-IN-79
  • HY-156912
    Tyrosine kinase-IN-7
    		Inhibitor 99.25%
    Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC50s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC50s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively.
    Tyrosine kinase-IN-7
  • HY-170665
    EGFR T790M/L858R-IN-9
    		Inhibitor
    EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC50 value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research.
    EGFR T790M/L858R-IN-9
  • HY-146127
    Grb2 SH2 domain inhibitor 1
    		Inhibitor
    Grb2 SH2 domain inhibitor 1 is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.
    Grb2 SH2 domain inhibitor 1
  • HY-169982
    EGFR-IN-136
    		Inhibitor
    EGFR-IN-136 (compound 21v) is a potent EGFR inhibitor with IC50 values of 20.2, 1.2, 2.3, 12.5 nM for EGFRWT, EGFRLR/TM, EGFR19D/TM/CS, EGFRLR/TM/CS, respectively. EGFR-IN-136 shows antiproliferative activity. EGFR-IN-136 shows antitumor activity and has the potential for the research of NSCLC.
    EGFR-IN-136
  • HY-N0211R
    Cyasterone (Standard)
    		Inhibitor
    Cyasterone (Standard) is the analytical standard of Cyasterone. This product is intended for research and analytical applications. Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.
    Cyasterone (Standard)
  • HY-139997
    DDC-01-163
    		Degrader
    DDC-01-163 is a mutant-selective allosteric PROTAC-based EGFR degrader, with an IC50 of 45 nM (Pink: EGFR ligand (HY-151048); Black: linker (HY-W008005); Blue: CRBN ligand (HY-14658)).
    DDC-01-163
  • HY-171252
    EGFR-IN-145
    		Inhibitor
    EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, EGFR-IN-145 has an inhibition rate of 52.7% on EGFR-wild type kinase.
    EGFR-IN-145
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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