2. Signaling Pathways
  3. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  4. EGFR

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

Related Products

PDF 3.8 MB

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-18957B
    Lifirafenib maleate
    		Inhibitor
    Lifirafenib (BGB-283) maleate 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 maleate
  • HY-161923
    EGFR-IN-120
    		Inhibitor
    EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFRL858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFRWT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFRL858R/T790M/C797S with an IC50 of 0.052 μM.
    EGFR-IN-120
  • HY-172621
    EGFR-IN-159
    		Inhibitor
    EGFR-IN-159 (compound 12), a dihydropyrimidine, is a potent EGFR inhibitor with an IC50 value of 29.00 nM. EGFR-IN-159 exhibits dose-dependent inhibition against EGFR and HER2. EGFR-IN-159 shows cytotoxicity against MCF-7 breast cancer cells and Vero cells with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. EGFR-IN-159 has no BBB permeation. EGFR-IN-159 shows appreciable anti-cancer activity.
    EGFR-IN-159
  • HY-168492
    TrxR/EGFR-IN-1
    		Inhibitor
    TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor. TrxR/EGFR-IN-1 is active against both Gefitinib (HY-50895)-sensitive and resistant lung cancers, effectively inhibiting tumor proliferation and promoting apoptosis. TrxR/EGFR-IN-1 promotes the degradation of GPX4 protein through autophagolysosomal and proteasomal pathways, leading to ferroptosis. In addition, TrxR/EGFR-IN-1 can induce endoplasmic reticulum stress and trigger immunogenic cell death. TrxR/EGFR-IN-1 can be used for the research of Gefitinib (HY-50895)-resistant lung cancer.
    TrxR/EGFR-IN-1
  • HY-149556
    MTX-241F
    		Inhibitor
    MTX-241F is a selective small molecule inhibitor targeting EGFR and PI3 kinase family members. MTX-241F is able to penetrate the blood-brain barrier and control tumor growth over the long term. MTX-241F exhibits radiosensitizing activity in patient-derived DIPG neurospheres and may be used in the study of diffuse intrinsic pontine glioma (DIPG).
    MTX-241F
  • HY-P991524
    MM-111
    		Inhibitor
    MM-111 is a bispecific antibody fusion protein targeting the ErbB2/ErbB3 oncogenic unit. MM-111 blocks activation of the PI3K pro-survival pathway. MM-111 binds to the ErbB2 receptor, which localizes the bispecific molecule to ErbB2 over-expressing tumor cells and promotes binding of the anti-ErbB3 arm to the ErbB3 receptor. MM-111 binding to ErbB3 results in inhibition of ErbB3 signaling by blocking the binding of the ErbB3 physiological ligand heregulin. MM-111 can be used for the study of ErbB2 over-expressing breast tumors.
    MM-111
  • HY-RS04211
    Egfr Rat Pre-designed siRNA Set A
    		Inhibitor

    Egfr Rat Pre-designed siRNA Set A contains three designed siRNAs for Egfr gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Egfr Rat Pre-designed siRNA Set A
  • HY-N0281R
    Daphnetin (Standard)
    		Inhibitor
    Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. 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-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.
    Daphnetin (Standard)
  • HY-163663
    AZ14133346
    		Inhibitor
    AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
    AZ14133346
  • HY-RS04466
    ERBB2 Human Pre-designed siRNA Set A
    		Inhibitor

    ERBB2 Human Pre-designed siRNA Set A contains three designed siRNAs for ERBB2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    ERBB2 Human Pre-designed siRNA Set A
  • HY-164056
    EGFR T790M/L858R-IN-8
    		Inhibitor 99.20%
    EGFR T790M/L858R-IN-8 (compound 9) is a potent inhibitor of EGFR targeting mutant EGFRT790M/L858R with an IC50 of 56.8 μM. The anti-proliferative effect of EGFR T790M/L858R-IN-8 on cancer cell lines A549, A431, and NHI-H1975 is not significant.
    EGFR T790M/L858R-IN-8
  • HY-161319
    EGFR-IN-104
    		Inhibitor
    EGFR-IN-104 (Compound A23) is an effective inhibitor of EGFR, with IC50 values of 0.33 μM and 0.133 μM against EGFRL858R/T790M and EGFRDel19/T790M/C797S, respectively. EGFR-IN-104 exhibits anticancer activity both in vitro and in vivo.
    EGFR-IN-104
  • HY-P99406A
    Petosemtamab (FUT8-KO)
    Petosemtamab (FUT8-KO) is an anti-EGFR/LGR5 monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Petosemtamab (HY-P99406) is an anti-EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to blockade of EGFR signaling and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the study of solid tumors such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC), etc.
    Petosemtamab (FUT8-KO)
  • HY-P991240
    CDX-3379
    		Inhibitor
    CDX-3379 is a humanized monoclonal antibody inhibitor targeting ErbB3. CDX-3379 binds to ErbB3, blocking the dimerization of ErbB3 with other receptors, thereby inhibiting the phosphorylation of ErbB3. CDX-3379 can inhibit the growth and proliferation of tumor cells. CDX-3379 is promising for research of tumors expressing ErbB3 and NRG1, such as HNSCC.
    CDX-3379
  • HY-168170
    EGFR/VEGFR2-IN-2
    		Inhibitor
    EGFR/VEGFR2-IN-2 (compound 4b) is an dual inhibitor VEGFR-2 and EGFR..
    EGFR/VEGFR2-IN-2
  • HY-170497
    EGFR-IN-140
    		Inhibitor
    EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with Ki of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC50 of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model.
    EGFR-IN-140
  • 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-P991571
    GC1118
    GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer.
    GC1118
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.