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

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

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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-W782083
    p-SCN-Bn-NOTA trihydrochloride
    		99.62%
    p-SCN-Bn-NOTA trihydrochloride is a macrocyclic chelator. p-SCN-Bn-NOTA trihydrochloride can be covalently coupled to molecules such as peptides through the thiocyanate group to form hexacoordinate copper (such as 64Cu) complexes. p-SCN-Bn-NOTA trihydrochloride specifically binds to GRPR or EGFR highly expressed on the surface of tumor cells, mediating tumor enrichment of radioactive probes. p-SCN-Bn-NOTA trihydrochloride can be used to study malignant tumors expressing GRPR or EGFR, such as prostate cancer and colorectal cancer.
    p-SCN-Bn-NOTA trihydrochloride
  • HY-108016
    Peruvoside
    		Inhibitor 99.32%
    Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib.
    Peruvoside
  • HY-131864
    SJF-1528
    		Degrader 99.71%
    SJF-1528 is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. SJF-1528 also degrades HER2 (Pink: ligand for target protein (HY-159047); Black: linker Tos-PEG2-CH2-Boc (HY-130532); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845)).
    SJF-1528
  • HY-10346A
    AV-412 free base
    		Inhibitor 98.33%
    AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
    AV-412 free base
  • HY-50896R
    Erlotinib (Standard)
    		Inhibitor
    Erlotinib (Standard) is the analytical standard of Erlotinib. This product is intended for research and analytical applications. 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 (Standard)
  • HY-12008R
    Erlotinib Hydrochloride (Standard)
    		Inhibitor
    Erlotinib (Hydrochloride) (Standard) is the analytical standard of Erlotinib (Hydrochloride). This product is intended for research and analytical applications. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib Hydrochloride (Standard)
  • HY-113599
    Isoprocurcumenol
    		Activator
    Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate EGFR signaling. Isoprocurcumenol increases the phosphorylation of ERK and AKT. Isoprocurcumenol promotes the proliferation of keratinocytes.
    Isoprocurcumenol
  • HY-126320
    EGFR-IN-8
    		Inhibitor 98.01%
    EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.
    EGFR-IN-8
  • HY-155079
    DZD1516
    		98.31%
    DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models.
    DZD1516
  • HY-100214
    EAI001
    		Inhibitor 99.88%
    EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer.
    EAI001
  • HY-10261S
    Afatinib-d6
    		Inhibitor ≥99.0%
    Afatinib-d6 is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor[1].
    Afatinib-d<sub>6</sub>
  • HY-P10224A
    G7-18NATE TFA
    		98.59%
    G7-18NATE TFA is a peptide inhibitor of Grb7. G7-18NATE TFA binds to the Grb7-SH2 domain with micromolar affinity (Kd = 18.1 μM). G7-18NATE TFA inhibits cell proliferation, motility, cell invasion and 3D culture formation in several cancer cell lines.
    G7-18NATE TFA
  • HY-153901
    PROTAC EGFR degrader 8
    		Inhibitor 98.90%
    PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader. PROTAC EGFR degrader 8 degrades EGFR in HCC827 cell with a DC50 of 15.56 nM. PROTAC EGFR degrader 8 inhibits H1975, PC-9, HCC827 cell growth with IC50s of 7.72 nM, 121.9 nM, 14.21 nM. PROTAC EGFR degrader 8 can be used for research of cancer, especially NSCLC.
    PROTAC EGFR degrader 8
  • HY-161536
    PROTAC EGFR degrader 9
    		Inhibitor 98.35%
    PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFRL858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)).
    PROTAC EGFR degrader 9
  • HY-117155
    PKI-166
    		Inhibitor 99.58%
    PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
    PKI-166
  • HY-50895R
    Gefitinib (Standard)
    		Inhibitor
    Gefitinib (Standard) is the analytical standard of Gefitinib. This product is intended for research and analytical applications. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
    Gefitinib (Standard)
  • HY-142512
    EGFR-IN-24
    		Inhibitor 98.71%
    EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively.
    EGFR-IN-24
  • HY-149530
    EGFR-IN-86
    		Inhibitor 99.92%
    EGFR-IN-86 (compound 4i) is an EGFR inhibitor (IC50: 1.5 nM) with high activity against glioblastoma. EGFR-IN-86 induces apoptosis and arrests the U87 cell cycle in the G2/M phase.
    EGFR-IN-86
  • HY-103566
    LY456236
    		Inhibitor 99.81%
    LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM.
    LY456236
  • HY-15801
    HG-14-10-04
    		Inhibitor 99.09%
    HG-14-10-04 is a potent ALK and mutant EGFR inhibitor with IC50s of 20 nM, 15.6 nM, 22.6 nM and 124.5 nM for ALK, EGFRLR/TM, EGFR19del/TM/CS and EGFRLR/TM/CS, respectively. HG-14-10-04 can be used to research anticancer.
    HG-14-10-04
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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