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-173501
    EGFR-IN-157
    		Inhibitor
    EGFR-IN-157 (compound IIB-5) is a potent EGFR inhibitor with an IC50 of 18.81 nM. EGFR-IN-157 can be used in the study of non-small cell lung cancer (NSCLC).
    EGFR-IN-157
  • HY-P10659
    Self-assembling peptide pY1
    Self-assembling peptide pY1 is a peptide that assemblies around cancer cells and targets EGFR. When co-cultured with Ovalbumin (OVA), pY1 can effectively block the endocytosis of OVA.
    Self-assembling peptide pY1
  • HY-164694
    Emupertinib
    		Inhibitor
    Emupertinib (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively.
    Emupertinib
  • HY-142679
    EGFR-IN-22
    		Inhibitor
    EGFR-IN-22 is a potent EGFR inhibitor with IC50s of 4.91 nM and 0.54 nM for wild type EGFR and EGFRL858R/T790M/C797S, respectively (CN112538072A, compound 243).
    EGFR-IN-22
  • HY-144055
    EGFR-IN-38
    		Inhibitor
    EGFR-IN-38 is a potent inhibitor of EGFR. EGFR-IN-38 is an anti-tumor agent with low toxic side effects. EGFR-IN-33 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-38 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 4).
    EGFR-IN-38
  • HY-152144
    EGFR-IN-75
    		Inhibitor
    EGFR-IN-75 is an EGFRWT and EGFRT790M inhibitor with IC50 values of 0.28 μM and 5.02 μM, respectively. EGFR-IN-75 shows anticancer and antioxidant activity.
    EGFR-IN-75
  • HY-151158
    EGFR/HER2-IN-7
    		Inhibitor
    EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM).
    EGFR/HER2-IN-7
  • HY-162482
    EGFR kinase inhibitor 5
    		Inhibitor
    EGFR kinase inhibitor 5 (Compound 4c) is an orally active inhibitor for epidermal growth factor receptor (EGFR) kinase, with IC50 of 18.35 μM. EGFR kinase inhibitor 5 induces apoptosis. EGFR kinase inhibitor 5 exhibits anticancer and anti-inflammatory activity with low toxicity (LD50 range: 500-2000 mg/kg).
    EGFR kinase inhibitor 5
  • HY-151377
    RET-IN-19
    		Inhibitor
    RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research.
    RET-IN-19
  • HY-P1828
    EGFRvIII peptide (PEPvIII)
    EGFRvIII peptide (PEPvIII) is a tumor-specific mutation that is widely expressed in glioblastoma multiforme (GBM) and other neoplasms and its expression enhances tumorigenicity. EGFRvIII peptide represents a truly tumor-specific target for antitumor immunotherapy.
    EGFRvIII peptide (PEPvIII)
  • HY-15268
    PP487
    		Inhibitor
    PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research.
    PP487
  • HY-50898S1
    Lapatinib-d7 dihydrochloride
    		Inhibitor
    Lapatinib-d7 dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride 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> dihydrochloride
  • HY-402309
    IGF-1R modulator 1
    		Modulator
    IGF-1R modulator 1 (Example 5) is an IGF-1R modulator, with EC50s of 0.29 μM (FGFR1), 0.25 μM (IGF1R), 0.34 μM (TrkA), 0.39 μM (TrkB). IGF-1R modulator 1 can be used for research of diseases characterised by impaired signalling of neurotrophins and/or other trophic factors, such as Alzheimer's disease.
    IGF-1R modulator 1
  • HY-168627
    EGFR-IN-135
    		Inhibitor
    EGFR-IN-135 (compound 3d) is a EGFR inhibitor with the IC50 of 0.086 μM. EGFR-IN-135 inhibitor cell growth and arrests the cell cycle at the S phase of reast cancer cell lines.
    EGFR-IN-135
  • HY-175011
    EGFR-IN-165
    		Inhibitor
    EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFRL858R/T790M and EGFRWT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma.
    EGFR-IN-165
  • HY-155118
    EGFR-IN-81
    		Inhibitor
    EGFR-IN-81 (Compound 10i) is an EGFR inhibitor. EGFR-IN-81 inhibits EGFR WT and L858R/T790M with IC50s 4.38 nM and 5.69 nM. EGFR-IN-81 has cytotoxic activity against MCF-7 and HCT116 cells with of 2.07 μM and 6.72 μM respectively.
    EGFR-IN-81
  • HY-P991159
    Ruzaltatug
    		Inhibitor
    Ruzaltatug is a humanized IgG1 antibody targeting ERBB3. The corresponding isotype control is: Human IgG1 kappa, Isotype Control (HY-P99001).
    Ruzaltatug
  • HY-147741
    DPPY
    		Inhibitor
    DPPY (compound 6) is a potent PTK inhibitor with IC50 values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).
    DPPY
  • HY-164490
    LS-106
    		Inhibitor
    LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model.
    LS-106
  • HY-163419
    HER2-IN-18
    		Inhibitor
    HER2-IN-18 is a HER2 inhibitor, with an IC50 less than 200 nM for HER-YVMA and HER-WT. HER2-IN-18 can be used for cancer research.
    HER2-IN-18
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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