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-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-P991588
    HLX-22
    		Antagonist
    HLX-22 is a humanized monoclonal antibody targeting HER2. HLX-22 induces apoptosis in HER2-overexpressing breast and gastric cancer cells combined with Trastuzumab (HY-P9907). HLX-22 has potent antitumor activity against advanced solid tumors.
    HLX-22
  • 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-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-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-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
  • HY-32721R
    Neratinib (Standard)
    		Inhibitor
    Neratinib (Standard) is the analytical standard of Neratinib. This product is intended for research and analytical applications. Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.
    Neratinib (Standard)
  • HY-164464
    BPI-15086
    		Inhibitor
    BPI-15086 an orally active, potent, irreversible mutant-selective inhibitor of both EGFR and T790M resistance mutations tyrosine kinase. BPI-15086 can be used for the research of non-small-cell lung cancer.
    BPI-15086
  • HY-101756
    SDZ281-977
    		98.00%
    SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.
    SDZ281-977
  • HY-15732
    BGB-102
    		Inhibitor 99.52%
    BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
    BGB-102
  • HY-21291
    SU-4313
    		Modulator 99.31%
    SU-4313 is a potent protein tyrosine kinases (PTKs) modulator with IC50s of 14.5 μM, 18.8 μM, 11 μM, 16.9 μM, 8.0 μM for PDGFR, FLK-1, EGFR, HER2 Kinase and IGF-1R, respectively. SU-4313 has the potential for modulating tyrosine kinase signal transduction in order to regulate abnormal cell proliferation.
    SU-4313
  • HY-19981B
    Derazantinib dihydrochloride
    		Inhibitor
    Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models.
    Derazantinib dihydrochloride
  • HY-100520
    EGFR-IN-2
    		Inhibitor
    EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
    EGFR-IN-2
  • HY-50895B
    Gefitinib dihydrochloride
    		Inhibitor
    Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
    Gefitinib dihydrochloride
  • HY-104066A
    Theliatinib tartrate
    Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Theliatinib tartrate
  • HY-10261D
    Afatinib oxalate
    		Inhibitor
    Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib oxalate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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