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-N14637
    Paeciloquinone C
    		Inhibitor
    Paeciloquinone C can inhibit the EGFR protein tyrosine kinase. Paeciloquinone C inhibits the V-abl protein tyrosine Kinase with an IC50 of 0.56 μM.
    Paeciloquinone C
  • HY-W740378
    1,2,3,4-Tetrahydro Staurosporin
    		Inhibitor
    1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC50=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC50=390 nM). It also binds to Janus kinase 3 (JAK3).
    1,2,3,4-Tetrahydro Staurosporin
  • HY-32718R
    Pelitinib (Standard)
    		Inhibitor
    Pelitinib (Standard) is the analytical standard of Pelitinib. This product is intended for research and analytical applications. Pelitinib (EKB-569;WAY-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 (Standard)
  • HY-153887
    HyT36(-Cl)
    		Control
    HyT36(-Cl) is the inactive control compound of HyT36, a small molecule hydrophobic tag compound that can be used in protein folding research.
    HyT36(-Cl)
  • HY-16069S
    Tucatinib-d6
    		Inhibitor
    Tucatinib-d6 (Irbinitinib-d6) is deuterium labeled Tucatinib. Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
    Tucatinib-d<sub>6</sub>
  • HY-50896S2
    Erlotinib-d4
    		Inhibitor
    Erlotinib-d4 (CP-358774-d4) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer. Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib-d<sub>4</sub>
  • HY-50898S4
    Lapatinib-d7
    		Inhibitor
    Lapatinib-d7 (GW572016-d7) is deuterium labeled Lapatinib. Lapatinib (GW572016) 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-d<sub>7</sub>
  • HY-123766
    EGFR-IN-99
    		Inhibitor
    EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC).
    EGFR-IN-99
  • HY-17499R
    EGFR-IN-12 (Standard)
    		Inhibitor
    EGFR-IN-12 (Standard) is the analytical standard of EGFR-IN-12. This product is intended for research and analytical applications. EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFRL858R and EGFRL861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
    EGFR-IN-12 (Standard)
  • HY-10322R
    Falnidamol (Standard)
    		Inhibitor
    Falnidamol (Standard) is the analytical standard of Falnidamol. This product is intended for research and analytical applications. Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
    Falnidamol (Standard)
  • HY-101820R
    Simotinib (Standard)
    		Inhibitor
    Simotinib (Standard) is the analytical standard of Simotinib. This product is intended for research and analytical applications. Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
    Simotinib (Standard)
  • HY-114667
    Lavendustin C6
    		Inhibitor
    Lavendustin C6 is a specific inhibitor of tyrosine kinase. Lavendustin C6 inhibits epidermal growth factor (EGF) receptor tyrosine kinase with an EC50 value of 0.05 μg/mL. Lavendustin C6 inhibits platelet-derived growth factor (PDGF)-induced inositol phosphate formation.
    Lavendustin C6
  • HY-135725
    D-69491 hydrochloride
    		Inhibitor
    D-69491 hydrochloride is a HER-2 tyrosine kinase inhibitor that reduces HER-2 phosphorylation, inhibits the proliferation of SKOV-3 cells, and has anticancer activity.
    D-69491 hydrochloride
  • HY-50895AR
    Gefitinib hydrochloride (Standard)
    		Inhibitor
    Gefitinib (hydrochloride) (Standard) is the analytical standard of Gefitinib (hydrochloride). This product is intended for research and analytical applications. Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity.
    Gefitinib hydrochloride (Standard)
  • HY-N14635
    Paeciloquinone A
    		Inhibitor
    Paeciloquinone A can inhibit EGFR protein tyrosine kinase. Paeciloquinone A inhibits the V-abl protein tyrosine kinase with an IC50 of 0.59 μM.
    Paeciloquinone A
  • HY-156872
    MTX-216
    		Inhibitor
    MTX-216 is a dual ATP-competitive inhibitor of PI3K and EGFR. MTX-216 cosuppresses Ki-67 and ribosomal S6 phosphorylation and induces apoptosis in NF1LOF cells. MTX-216 suppresses the activity of SYK kinase, with an IC50 of 281 nM. MTX-216 is used in the research of Melanoma.
    MTX-216
  • HY-N14636
    Paeciloquinone B
    		Inhibitor
    Paeciloquinone B can inhibit the EGFR protein tyrosine kinase.
    Paeciloquinone B
  • HY-146262
    LDC0496
    		Inhibitor
    LDC0496 is a potent and selective EGFR inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome.
    LDC0496
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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