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

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

Related Products

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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-147407
    Imbotolimod
    		Inhibitor
    Imbotolimod, immunoglobulin G1-kappa, is a humanized monoclonal antibody with anti-ERBB2 and antineoplastic activity. Imbotolimod is a derivative of telratolimod.
    Imbotolimod
  • HY-147303
    Sacibertinib
    		Inhibitor
    Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity.
    Sacibertinib
  • HY-123726
    ErbB-1/ErbB-2 tyrosine kinase-IN-1
    ErbB-1/ErbB-2 tyrosine kinase-IN-1 is a dual ErbB-1/ErbB-2 tyrosine kinase inhibitor with IC50 values of 0.027 μM and 0.026 μM. ErbB-1/ErbB-2 tyrosine kinase-IN-1 targets the ATP binding region of ErbB-1 and ErbB-2 tyrosine kinases. ErbB-1/ErbB-2 tyrosine kinase-IN-1 inhibits cancer cells proliferation.
    ErbB-1/ErbB-2 tyrosine kinase-IN-1
  • HY-10407G
    SU 5402 (GMP)
    		Inhibitor
    SU 5402 (GMP) is SU 5402 (HY-10407) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
    SU 5402 (GMP)
  • HY-174232
    EGFR/CA-IX-IN-1
    		Inhibitor
    EGFR/CA-IX-IN-1 (Compound 14) is a dual inhibitor against epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX) with IC50 values of 5.92 nM and 63 nM, respectively. EGFR/CA-IX-IN-1 shows strong cytotoxicity against breast cancer cells (MDA-MB-231, MCF-7) with IC50 values of 5.78 μM and 8.05 μM, respectively. EGFR/CA-IX-IN-1 inhibits the catalytic activity of CA-IX, up-regulates BAX/Bcl-2, activates caspases, and arrests the cell cycle at the G1 phase. EGFR/CA-IX-IN-1 is promising for research of breast cancer.
    EGFR/CA-IX-IN-1
  • HY-P991243
    MP-RM-1
    		Inhibitor
    MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a Kd value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells.
    MP-RM-1
  • HY-171884
    BI-8128
    		Inhibitor
    BI-8128 is a potent EGFR inhibitor, with IC50 values of 12, 6.7, 22, 10, and 3 nM against wild-type, T790M, C797S, T790M/C797S, and L858R/T790M/C797S mutant EGFR, respectively. BI-8128 significantly inhibits the proliferation of Ba/F3 and PC-9 drug-resistant mutant cells. BI-8128 is applicable for the research of non-small cell lung cancer.
    BI-8128
  • HY-174826
    EGFR-IN-164
    		Inhibitor
    EGFR-IN-164 (Compound 4) is a selective and covalent allosteric EGFR inhibitor. EGFR-IN-164 significantly inhibits the activity of EGFRL858R/T790M/C797S kinase (IC50: 48.1 nM) and proliferation of of EGFR-mutant cells. EGFR-IN-164 can be used for drug resistance of cancer research.
    EGFR-IN-164
  • HY-18963R
    Lavendustin A (Standard)
    		Inhibitor
    Lavendustin A (Standard) is the analytical standard of Lavendustin A. This product is intended for research and analytical applications. Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis[1][2].
    Lavendustin A (Standard)
  • HY-E70696
    EGFR C797S/L858R Recombinant Human Active Protein Kinase
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR C797S/L858R protein that can be used to study EGFR C797S/L858R-related functions.
    EGFR C797S/L858R Recombinant Human Active Protein Kinase
  • HY-143733
    HER2-IN-5
    		Inhibitor
    HER2-IN-5 is a potent and orally active HER-2 inhibitor, example 10, extracted from patent WO2021164697.
    HER2-IN-5
  • HY-P991092A
    IBI-334 (FUT8-KO)
    		Inhibitor
    IBI-334 (FUT8-KO) is a bispecific B7-H3 and EGFR antibody that has knocked out the fucosyltransferase 8 gene (FUT8). IBI-334 (FUT8-KO) has an EGFR arm for signal blocking and is coupled with a fine-tuned B7-H3 arm with the best affinity and binding domain. IBI-334 (FUT8-KO), compared to IBI-334 (HY-P991092), has enhanced antibody-mediated cytotoxicity (ADCC) effect. IBI-334 (FUT8-KO) has wide applications in many EGFR-driven solid tumors.
    IBI-334 (FUT8-KO)
  • HY-172091
    CZY43
    		Degrader
    CZY43 is a HER3 degrader. CZY43 can effectively induce HER3 degradation in a dose- and time-dependent manner in breast cancer SKBR3 cells. CZY43 potently inhibits HER3-dependent signaling and cancer cell growth and outperforms Bosutinib (HY-10158).
    CZY43
  • HY-144053
    EGFR-IN-36
    		Inhibitor
    EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research.
    EGFR-IN-36
  • HY-183123
    EGFR T790M/FAK-IN-1
    		Inhibitor
    EGFR T790M/FAK-IN-1 is a dual inhibitor of EGFRT790M and FAK, with an IC50 of 99.1 nM against EGFRT790M and an IC50 of 117.7 nM against FAK. EGFR T790M/FAK-IN-1 can be used for research on pancreatic cancer, drug-resistant breast cancer, and drug-resistant lung cancer.
    EGFR T790M/FAK-IN-1
  • HY-120412
    SKLB188
    		Inhibitor
    SKLB188 is an orally active and potent epidermal growth factor receptor (EGFR) inhibitor (IC50=5 nM). SKLB188 suppresses MEK/Erk and Akt/mTOR signaling pathways to inhibit head and neck squamous cell carcinoma (HNSCC) proliferation and induce caspase-dependent apoptosis. SKLB188 is promising for research of EGFR-overexpressing solid tumors.
    SKLB188
  • HY-176938A
    iAfaPhos1
    iAfaPhos1 is a FKBP12F36V epimer ligand. iAfaPhos1 leads to reduced dephosphorylation of EGFR at pY1068 and pY845 sites. iAfaPhos1 has anticancer activity against non-small cell lung cancer.
    iAfaPhos1
  • HY-16558R
    Butein (Standard)
    		Inhibitor
    Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0794BR
    AZ7550 Mesylate (Standard)
    		Inhibitor
    AZ7550 Mesylate (Standard) is the analytical standard of AZ7550 Mesylate. This product is intended for research and analytical applications. AZ7550 Mesylate is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
    AZ7550 Mesylate (Standard)
  • HY-50898S3
    Lapatinib-d4-1
    		Inhibitor
    Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active 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>-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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