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-19617B
    EGFR-IN-1 TFA
    Inhibitor 99.38%
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
    EGFR-IN-1 TFA
  • HY-B0794
    AZ7550
    Inhibitor
    AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
    AZ7550
  • HY-172429
    Enozertinib
    Inhibitor
    Enozertinib is the inhibitor for EGFR that exhibits antineoplastic activity.
    Enozertinib
  • HY-P3744
    pp60v-src Autophosphorylation site
    99.93%
    pp60v-src Autophosphorylation site is a synthetic peptide. pp60v-src Autophosphorylation site can be used for various biochemical studies.
    pp60v-src Autophosphorylation site
  • HY-P99854A
    Disitamab (powder)
    Inhibitor 98.44%
    Disitamab (RC48-0) (powder) is a humanized monoclonal antibody targeting HER2. Disitamab (powder) can be used in the synthesis of antibody-drug conjugates (ADCs), Disitamab vedotin (Disitamab vedotin (HY-P9985)).
    Disitamab (powder)
  • HY-U00002
    ZD-4190
    Inhibitor 98.08%
    ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
    ZD-4190
  • HY-P2673A
    Lys-Arg-Thr-Leu-Arg-Arg acetate
    Lys-Arg-Thr-Leu-Arg-Arg (KRTLRR) acetate is a hexapeptide. Lys-Arg-Thr-Leu-Arg-Arg acetate is a substrate of EGF receptor protein kinase C and can be used to measure protein kinase C activity.
    Lys-Arg-Thr-Leu-Arg-Arg acetate
  • HY-P99969
    Inetetamab
    Inhibitor
    Inetetamab is a monoclonal antibody binding to domain IV of HER2 receptor. Inetetamab alone or together with tyrosine kinase inhibitors has antitumor activities.
    Inetetamab
  • HY-P99672
    Istiratumab
    Inhibitor 98.45%
    Istiratumab (M-6495) is bispecific monoclonal antibody targeting IGF-1R and ErbB3. Istiratumab induces IGF-1R and ErbB3 receptor degradation through the proteasome pathway Istiratumab can be used for research of cancers.
    Istiratumab
  • HY-150610
    EGFR-IN-69
    Inhibitor 99.58%
    EGFR-IN-69 (compound 17g) is a potent EGFR inhibitor, with IC50 values of 4.3, 6.6 and 25.6 nM against EGFRL858R/T790M/C797S, EGFRL858R/T790M, and EGFR19del/T790M/C797S, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research.
    EGFR-IN-69
  • HY-103439
    GW583340 dihydrochloride
    Inhibitor
    GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50: 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride reverses ABCG2- and ABCB1-mediated drug resistance. GW 583340 dihydrochloride has anti-cancer activity.
    GW583340 dihydrochloride
  • HY-164307
    Pebezertinib
    Inhibitor 99.56%
    Pebezertinib (BLU 451) is an orally active inhibitor for EGFR. Pebezertinib exhibits the ability to penetrate the central nervous system (CNS). Pebezertinib can be used for research about non-small cell lung cancer carrying EGFR exon 20 insertion.
    Pebezertinib
  • HY-101522
    CHMFL-EGFR-202
    Inhibitor 99.75%
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ~10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
    CHMFL-EGFR-202
  • HY-158149
    T-1-PMPA
    Inhibitor 99.70%
    T-1-PMPA is a potent EGFR inhibitor with apoptotic properties. T-1-PMPA effectively inhibits EGFRWT and EGFR790m, with IC50 values of 86 nM and 561.73 nM, respectively.
    T-1-PMPA
  • HY-112823R
    Almonertinib (Standard)
    Inhibitor
    Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
    Almonertinib (Standard)
  • HY-B0794S
    AZ7550-d5
    Inhibitor
    AZ7550-d5 is the deuterium labeled AZ7550?(HY-B0794). AZ7550, an active metabolite of Osimtinib (AZD9291; HY-15772), inhibits the activity of?IGF1R?with an?IC50?of 1.6 μM.
    AZ7550-d<sub>5</sub>
  • HY-157582
    MS39N
    Control 98.0%
    MS39N (compound 27) is a negative control for MS39 that binds EGFR without inducing degradation.
    MS39N
  • HY-138751A
    limertinib diTFA
    Inhibitor ≥98.0%
    limertinib (ASK120067) diTFA is a potent and orally active inhibitor of EGFRT790M (IC50: 0.3 nM) with selectivity over EGFRWT (IC50: 6.0 nM). limertinib diTFA is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC).
    limertinib diTFA
  • HY-164476
    ES-072
    Inhibitor 98.05%
    ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells.
    ES-072
  • HY-12872A
    Nazartinib mesylate
    Inhibitor
    Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.
    Nazartinib mesylate
Cat. No. Product Name / Synonyms Species Source
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