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-147798
    EGFR/HER2/CDK9-IN-3
    		Inhibitor
    EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 191.08, 132.65, and 113.98 nM, respectively. EGFR/HER2/CDK9-IN-3 exhibits remarkable antitumor activity.
    EGFR/HER2/CDK9-IN-3
  • HY-172156
    EGFR-TK-IN-5
    		Inhibitor
    EGFR-TK-IN-5 (Compound NCE 2) is a thiazolyl-pyrazoline derivative. EGFR-TK-IN-5 exhibits strong inhibitory activity and stability against EGFR. EGFR-TK-IN-5 can be used in the study of cancer.
    EGFR-TK-IN-5
  • HY-P11752
    Cyclo(KLARLLT)
    		Ligand
    Cyclo (KLARLLT) is an EGFR ligand with a Kd value of 1.16 μM. Cyclo (KLARLLT) binds to domain I of EGFR and interacts with both the open and closed conformations of EGFR. Cyclo (KLARLLT) is a modified variant of LARLLT (HY-P11078). Cyclo (KLARLLT) can be used in the research of colorectal cancer.
    Cyclo(KLARLLT)
  • HY-162148
    HNPMI
    		Inhibitor 99.57%
    HNPMI is an inhibitor of EGFR and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis.
    HNPMI
  • HY-172897
    EGFR/DHFR-IN-2
    		Inhibitor
    EGFR/DHFR-IN-2 (9b) is a dual h-DHFR/EGFRTK inhibitor, with IC50 values of 0.192 μM and 0.109 μM for h-DHFR and EGFR, respectively. EGFR/DHFR-IN-2 (9b) halts the cell cycle at the G1/S phase and induces apoptosis. EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. EGFR/DHFR-IN-2 (9b) can be used in the cancer research.
    EGFR/DHFR-IN-2
  • HY-142519
    EGFR-IN-27
    		Inhibitor
    EGFR-IN-27 is a potent EGFR inhibitor with IC50s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511).
    EGFR-IN-27
  • HY-P991967
    AVID100 Antibody
    		Inhibitor
    AVID100 (MAB100) Antibody is a monoclonal antibody inhibitor targeting EGFR, which can be used to synthesize a novel antibody-drug conjugate (ADC) molecule AVID100. AVID100 Antibody is applicable to relevant research on breast cancer, head and neck cancer, and lung cancer.
    AVID100 Antibody
  • HY-147796
    EGFR/HER2/CDK9-IN-1
    		Inhibitor
    EGFR/HER2/CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 90.17, 131.39, and 67.04 nM, respectively. EGFR/HER2/CDK9-IN-1 exhibits remarkable antitumor activity.
    EGFR/HER2/CDK9-IN-1
  • HY-162602
    EGFR-IN-115
    		Inhibitor
    EGFR-IN-115 (H-13) is an EGFR inhibitor, with IC50 of 395.2 nM. EGFR-IN-115 can be used in anti-cancer research.
    EGFR-IN-115
  • HY-172179
    EGFR/VEGFR2-IN-5
    		Inhibitor
    EGFR/VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2 with an IC50 value of 1.15 µM for VEGFR2 and an IC50 value of 0.28 μM for EGFRT790M. EGFR/VEGFR2-IN-5 has significant anticancer activity.
    EGFR/VEGFR2-IN-5
  • HY-163418
    HER2-IN-17
    		Inhibitor
    HER2-IN-17 (Compound 2) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-17 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC).
    HER2-IN-17
  • HY-162623
    EGFR/HER2-IN-15
    		Inhibitor
    EGFR/HER2-IN-15, a dihydropyrimidine, is a potent EGFR/HER2 inhibitor. EGFR/HER2-IN-15 significantly inhibits EGFRwt activity with an IC50 of 37.21 nM. EGFR/HER2-IN-15 has anticaner effects.
    EGFR/HER2-IN-15
  • HY-171443
    Lyso-Monosialoganglioside GM3
    		Inhibitor
    Lyso-Monosialoganglioside GM3 (Lyso-GM3) is an analogue of Ganglioside GM3 (HY-114456) with antitumor activities. Lyso-Monosialoganglioside inhibits EGF-induced increases in EGFR kinase activity in A431 epithelial cancer cells.
    Lyso-Monosialoganglioside GM3
  • HY-144044
    EGFR-IN-30
    		Inhibitor
    EGFR-IN-30 is a potent EGFR inhibitor with IC50s of 1-10 nM, <1 nM for EGFR (WT), EGFR (L858R/T790M/C797S), respectively. EGFR-IN-30 has potential for cell proliferative diseases, such as cancer research.
    EGFR-IN-30
  • HY-163860
    EGFR-TK-IN-3
    		Inhibitor
    EGFR-TK-IN-3 (3) is an EGFR TK inhibitor, with an IC50 of 2.33 μM against Erlotinib (HY-50896)-resistant A549 cells.
    EGFR-TK-IN-3
  • HY-153557
    HER2-IN-13
    		Inhibitor
    HER2-IN-13 (Compound 33) is an HER2 inhibitor with an IC50 of 8 nM. HER2-IN-13 also inhibits wt-EGFR with an IC50 of 0.40 μM.
    HER2-IN-13
  • HY-172104
    EGFR-IN-143
    		Inhibitor
    EGFR-IN-143 (Compound 5f) is a potent EGFR inhibitor with an IC50 value of 0.15 μM. EGFR-IN-143 induces apoptosis by arresting the cell cycle in the G2/M phase. EGFR-IN-143 has antitumor activity.
    EGFR-IN-143
  • HY-157912
    EGFR-IN-102
    		Inhibitor
    EGFR-IN-102 (compound 6) is an oral active EGFR inhibitor with the IC50 of 2 nM, and can be used for study of non-small-cell lung cancer.
    EGFR-IN-102
  • HY-179529
    EGFR/InhA-IN-1
    		Inhibitor
    EGFR/InhA-IN-1 (Compound 15) is an inhibitor of the anti-cancer target EGFR tyrosine kinase (1M17) (Ki = 0.05 μM) and the anti-tuberculosis target InhA enzyme (1OUZ) (Ki = 0.02 μM). EGFR/InhA-IN-1 exhibits anti-proliferative activity against A549 cells, with an IC50 of 10.38 μM. EGFR/InhA-IN-1 has inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 6.25 μM. EGFR/InhA-IN-1 can be used for research on non-small cell lung cancer and Mycobacterium tuberculosis infection.
    EGFR/InhA-IN-1
  • HY-141486A
    PROTAC PARP/EGFR ligand 1
    PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology.
    PROTAC PARP/EGFR ligand 1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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