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-N2450R
    Sulforaphene (Standard)
    Inhibitor
    Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10-4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals.
    Sulforaphene (Standard)
  • HY-32718S
    Pelitinib-d6
    Pelitinib-d6 (EKB-569-d6) is the deuterium labeled Pelitinib. Pelitinib (EKB-569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
    Pelitinib-d6
  • HY-164919
    Calotatug ginistinag
    Inhibitor
    Calotatug ginistinag (XMT-2056) is an antibody-drug conjugate targeting HER2, with an effective payload connected via a linker (LP, HY-148067) to a STING agonist (STING agonist-20, HY-148068), and has potential immune activation and anticancer activity.
    Calotatug ginistinag
  • HY-168305
    EGFR ligand-11
    EGFR ligand-11 is a target protein ligand for EGFR and can be used to synthesize PROTAC MS154 (HY-141640).
    EGFR ligand-11
  • HY-19909A
    NRC-2694-A
    Inhibitor
    NRC-2694-A is an orally effective EGFR tyrosine kinase inhibitor. NRC-2694-A can be used in the study of malignant squamous cell carcinoma (HNSCC).
    NRC-2694-A
  • HY-16069AR
    Tucatinib hemiethanolate (Standard)
    Inhibitor
    Tucatinib (hemiethanolate) (Standard) is the analytical standard of Tucatinib (hemiethanolate). This product is intended for research and analytical applications. Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
    Tucatinib hemiethanolate (Standard)
  • HY-135727
    PF-6422899
    Inhibitor
    PF-6422899 is an inhibitor for EGFR, that it selectively binds to EGFR and SOAT1 in nanomolar levels.
    PF-6422899
  • HY-P991092
    IBI-334
    Inhibitor
    IBI-334 is a bispecific B7-H3 and EGFR antibody. IBI-334 has an EGFR arm for signal blockage and is coupled with a fine-tuned B7-H3 arm with optimal affinity and binding domain. IBI-334 is afucosylated to enhance its antibody-mediated cell cytotoxicity (ADCC) effects. IBI-334 has a wide range of applications in many EGFR-driven solid tumors.
    IBI-334
  • HY-100064R
    O-Desmethyl gefitinib (Standard)
    Inhibitor
    O-Desmethyl gefitinib (Standard) is the analytical standard of O-Desmethyl gefitinib. This product is intended for research and analytical applications. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays.
    O-Desmethyl gefitinib (Standard)
  • HY-N14349
    Asterriquinone
    Inhibitor
    Asterriquinone (ARQ), a Asterriquinone analog, is a Grb-2 binding inhibitor. Asterriquinone inhibits the Grb-2 binding activity to tyrosine phosphorylated EGFR, with an IC50 of 8.37 μM. Asterriquinone is a HIV1 reverse transcriptase inhibitor with a Ki of 2.3 μM. Asterriquinone also inhibits Grb-7 and PLC-γ binding activities..
    Asterriquinone
  • HY-104065BR
    Pyrotinib dimaleate (Standard)
    Inhibitor
    Pyrotinib dimaleate (Standard) is the analytical standard of Pyrotinib dimaleate. This product is intended for research and analytical applications. Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
    Pyrotinib dimaleate (Standard)
  • HY-158829
    SSOe26 sodium
    SSOe26 sodium is a 15mer antisense oligonucleotide targeting?HER4. SSOe26 sodium induces exon 26 skipping, leading to the generation of a novel mRNA transcript that excludes exon 26 (CYT2 isoform). SSOe26 sodium decreases tumour growth in mouse xenografts.
    SSOe26 sodium
  • HY-15729R
    Rociletinib (Standard)
    Inhibitor
    Rociletinib (Standard) is the analytical standard of Rociletinib. This product is intended for research and analytical applications. Rociletinib (CO-1686) 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 (Standard)
  • HY-164527
    Si306
    Inhibitor
    Si306 is a Src inhibitor with antitumor activity. Si306 reduces the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), and inhibits the invasion of human glioblastoma (GBM).
    Si306
  • HY-79077R
    Osimertinib dimesylate (Standard)
    Inhibitor
    Osimertinib (dimesylate) (Standard) is the analytical standard of Osimertinib (dimesylate). This product is intended for research and analytical applications. Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
    Osimertinib dimesylate (Standard)
  • HY-10367AR
    Canertinib dihydrochloride (Standard)
    Inhibitor
    Canertinib (dihydrochloride) (Standard) is the analytical standard of Canertinib (dihydrochloride). This product is intended for research and analytical applications. Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice.
    Canertinib dihydrochloride (Standard)
  • HY-103443A
    HKI-357 dimaleate
    Inhibitor
    HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 dimaleate suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
    HKI-357 dimaleate
  • HY-10261BR
    (E/Z)-Afatinib (Standard)
    Inhibitor
    (E/Z)-Afatinib (Standard) is the analytical standard of (E/Z)-Afatinib. This product is intended for research and analytical applications. (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.
    (E/Z)-Afatinib (Standard)
  • HY-N14640
    Paeciloquinone F
    Inhibitor
    Paeciloquinone F can inhibit the EGFR protein tyrosine kinase.
    Paeciloquinone F
  • HY-50898AR
    Lapatinib ditosylate (Standard)
    Inhibitor
    Lapatinib (ditosylate) (Standard) is the analytical standard of Lapatinib (ditosylate). This product is intended for research and analytical applications. Lapatinib ditosylate (GW572016 ditosylate) 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 ditosylate (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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