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-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-123952
    RTC-5
    		Inhibitor 99.37%
    RTC-5 (TRC-382) is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.
    RTC-5
  • HY-103566
    LY456236
    		Inhibitor 99.57%
    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-144304
    PROTAC EGFR degrader 2
    		Inhibitor
    PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC.
    PROTAC EGFR degrader 2
  • HY-161537
    EGFR ligand-9
    		Inhibitor 98.80%
    EGFR ligand-9 is an EGFR ligand. EGFR ligand-9 can be used for synthesis of PROTAC EGFR degrader 9 (HY-161536).
    EGFR ligand-9
  • HY-P99461
    Barecetamab
    		Inhibitor
    Barecetamab (ISU-104) is a fully human anti-ErbB3 monoclonal antibody. Barecetamab can be used for the research of recurrent/metastatic (R/M) head and neck squamous cell carcinoma (HNSCC).
    Barecetamab
  • HY-N1166
    Tephrosin
    		98.02%
    Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors.
    Tephrosin
  • HY-101042
    AG-494
    		Inhibitor 98.69%
    AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
    AG-494
  • HY-P1828A
    EGFRvIII peptide (PEPvIII) TFA
    		98.73%
    EGFRvIII peptide (PEPvIII) TFA is a tumor-specific mutation that is widely expressed in glioblastoma multiforme (GBM) and other neoplasms and its expression enhances tumorigenicity. EGFRvIII peptide TFA represents a truly tumor-specific target for antitumor immunotherapy.
    EGFRvIII peptide (PEPvIII) TFA
  • HY-P99306
    Modotuximab
    		Inhibitor 99.08%
    Modotuximab (DS 1024) is an IgG1κ-type chimeric antibody targeting human EGFR protein. Modotuximab binds non-overlapping epitopes on domain III of EGFR, a domain that is intact in EGFRvIII. Modotuximab has antitumor activity in vivo.
    Modotuximab
  • HY-161408
    GePhos1
    		98.88%
    GePhos1, a EGFR-targeting PhosTAC (phosphorylation targeting chimera), induces EGFR dephosphorylation. GePhos1 induces apoptosis.
    GePhos1
  • HY-157480
    EGFR/AURKB-IN-1
    		Inhibitor 99.43%
    EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of L858R EGFR and AURKB with IC50s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research.
    EGFR/AURKB-IN-1
  • HY-13984
    Mutant EGFR inhibitor
    		Inhibitor 99.40%
    Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M.
    Mutant EGFR inhibitor
  • HY-146349
    PROTAC EGFR degrader 4
    		Inhibitor 99.70%
    PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.
    PROTAC EGFR degrader 4
  • HY-124674A
    CCT365623 hydrochloride
    		Inhibitor 98.07%
    CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties.
    CCT365623 hydrochloride
  • HY-163094
    EGFR-IN-95
    		Inhibitor 98.76%
    EGFR-IN-95 (compound 5j) is an 2,4-diaminonicotinamide derivative. EGFR-IN-95 has potent inhibitory activity against EGFR del19/T790M/C797S and L858R/T790M/C797S.
    EGFR-IN-95
  • HY-135805B
    (Rac)-JBJ-04-125-02 acetate
    (Rac)-JBJ-04-125-02 acetate is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, selective mutagenesis, allosteric and orally active EGFR inhibitor.
    (Rac)-JBJ-04-125-02 acetate
  • HY-101450
    PF-6274484
    		Inhibitor 98.76%
    PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively.
    PF-6274484
  • HY-147858
    PROTAC EGFR degrader 7
    		Inhibitor 99.99%
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research. PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC EGFR degrader 7
  • HY-138916
    PF-06672131
    		Inhibitor 99.47%
    PF-06672131 is an alkynylated afatinib derivative and a small molecule probe that is reactive to cysteine. PF-06672131 is an inhibitor of epidermal growth factor receptor (EGFR) kinase that targets the ATP pockets of EGFR. PF-06672131 can be used for activity-based protein profiling studies.
    PF-06672131
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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