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-N0280R
    Corosolic acid (Standard)
    Corosolic acid (Standard) is the analytical standard of Corosolic acid. This product is intended for research and analytical applications. Corosolic acid (Colosolic acid) isolated from the fruit of Cratoegus pinnatifida var. psilosa, was reported to have anticancer activity. Corosolic acid induces cancer cell apoptosis.
    Corosolic acid (Standard)
  • HY-158178
    EGFR T790M/L858R-IN-7
    		Inhibitor
    EGFR T790M/L858R-IN-7 (Compound 72) is a novel pyrimidine compound that inhibits the EGFR T790M and L858R mutation with a high efficacy (93% inhibition rate at 0.05 μM). EGFR T790M/L858R-IN-7 functions by specifically binding to the kinase domain of EGFR, thereby inhibiting its phosphorylation activity.
    EGFR T790M/L858R-IN-7
  • HY-P991244
    REGN-1400
    		Inhibitor
    REGN-1400 is a humanized monoclonal antibody inhibitor targeting ErbB3. REGN-1400 reduces tumor cell proliferation by inhibiting ErbB3 and blocking related signaling pathways. REGN-1400 is promising for research of solid tumors such as non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and squamous cell carcinoma of the head and neck (SCCHN) .
    REGN-1400
  • HY-143874
    HER2-IN-7
    		Inhibitor
    HER2-IN-7 is a potent inhibitor of HER2. Deregulation of ErbB family signalling modulates proliferation, invasion, metastasis, angiogenesis, and tumour cell survival. HER2-IN-7 has the potential for the research of diseases associated ErbBs (especially HER2), including cancer (extracted from patent WO2019214634A1, compound 23).
    HER2-IN-7
  • HY-163377
    AZ5385
    		Inhibitor
    AZ5385 is an EGFR-tyrosine kinase inhibitor. AZ5385 is a HRV-2 virus blocker, with EC50 of 0.35 µM. AZ5385 affects the late stage of viral life cycle.
    AZ5385
  • HY-173500
    MG-3C
    		Inhibitor
    MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer.
    MG-3C
  • HY-112405
    BPIQ-I
    		Inhibitor
    BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively.
    BPIQ-I
  • HY-161269
    EGFR-IN-101
    		Inhibitor
    EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a EGFR inhibitor. The IC50 values for EGFRL858R/T790M/C797S and Ba/F3-EGFRL858R/T790M/C797S are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC).
    EGFR-IN-101
  • HY-161136
    EGFR/STAT3-IN-1
    		Inhibitor
    EGFR/STAT3-IN-1 (Compound 5k) is a dual inhibitor of EGFR/STAT3 with IC50 values for EGFR and STAT3 are 41 and 3.34 nM, respectively. EGFR/STAT3-IN-1 has antitumor activity.
    EGFR/STAT3-IN-1
  • HY-10261AR
    Afatinib dimaleate (Standard)
    		Inhibitor
    Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate 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 dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib dimaleate (Standard)
  • HY-144445
    NSC114126
    		Inhibitor
    NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases.
    NSC114126
  • HY-163420
    HER2-IN-16
    		Inhibitor
    HER2-IN-16 (Compound 14) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-16 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC).
    HER2-IN-16
  • HY-147995
    EGFR-IN-64
    		Inhibitor
    EGFR-IN-64 (Compound 3c) is a potent EGFR inhibitor with an IC50 of 0.33 μM. EGFR-IN-64 shows anticancer activity.
    EGFR-IN-64
  • HY-146474
    EGFR-IN-54
    		Inhibitor
    EGFR-IN-54 (Compound 3c) is a potent EGFR inhibitor with an IC50 of 1.623 µM. EGFR-IN-54 shows cytotoxic activity against cancer cell lines.
    EGFR-IN-54
  • HY-169568
    EGFR-IN-147
    		Inhibitor
    EGFR-IN-147 (compound ID-5841161) is a potent inhibitor of EGFR, with the inhibition rate of 14% at 1 μM. EGFR-IN-147 has the potential for the research of cancer.
    EGFR-IN-147
  • HY-171958
    PROTAC EGFR degrader 12
    		Degrader
    PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM.
    PROTAC EGFR degrader 12
  • HY-18213
    EGFR-IN-9
    		Inhibitor 98.84%
    EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.
    EGFR-IN-9
  • HY-155178
    Antiproliferative agent-34
    		Inhibitor
    Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values < 10 nM) under hypoxic condition.
    Antiproliferative agent-34
  • HY-172961
    EGFR-IN-162
    		Inhibitor
    EGFR-IN-162 (compound 20) is a potent EGFR inhibitor. EGFR-IN-162 increases early and late apoptosis and necrosis. EGFR-IN-162 is promising for research of breast cancer.
    EGFR-IN-162
  • HY-120857
    BPIQ-II hydrochloride
    		Inhibitor
    BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC50=8 pM). It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR.
    BPIQ-II hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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