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-158969
    EGFR-IN-113
    		Inhibitor
    EGFR-IN-113 (compound II-1) is an EGFR kinase inhibitor with an IC50 of 14.79 μM. EGFR-IN-113 can induce apoptosis and inhibit cell proliferation by downregulating Akt and Erk1/2 signaling. EGFR-IN-113 can be used for research in EGFR-driven cancers, such as lung cancer, pancreatic cancer, and breast cancer.
    EGFR-IN-113
  • HY-147826
    EGFR-IN-60
    		Inhibitor
    EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFRWT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio.
    EGFR-IN-60
  • HY-P10793
    Cyclic(YCDGFYACYMDV)
    		Inhibitor
    Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model.
    Cyclic(YCDGFYACYMDV)
  • HY-157402
    Topoisomerase II/EGFR-IN-1
    Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer.
    Topoisomerase II/EGFR-IN-1
  • HY-175608
    EGFR-IN-171
    		Inhibitor
    EGFR-IN-171 is an EGFR inhibitor with an IC50 value of 0.19 μM. EGFR-IN-171 also inhibits vascular endothelial growth factor 2 (VEGFR-2) with an IC50 value of 31.65 μM. EGFR-IN-171 can induce apoptosis and G2/M phase cell cycle arrest. EGFR-IN-171 can be used for cancer research, such as liver and breast cancer.
    EGFR-IN-171
  • HY-13050A
    Sapitinib fumarate
    		Inhibitor
    Sapitinib fumarate is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
    Sapitinib fumarate
  • HY-153744
    JGK-068S
    		Inhibitor
    JGK-068S (compound I) is a potent EGFR inhibitor.
    JGK-068S
  • HY-175257
    Theophylline-platinum(IV) prodrug-1
    		Inhibitor
    Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.
    Theophylline-platinum(IV) prodrug-1
  • HY-178448
    EGFR-IN-178
    		Inhibitor
    EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC).
    EGFR-IN-178
  • HY-158175
    EGFR T790M/L858R-IN-4
    		Inhibitor
    EGFR T790M/L858R-IN-4 (Example 14) is a potent EGFRT790M/L858R inhibitor with anticancer effects.
    EGFR T790M/L858R-IN-4
  • HY-173492
    EGFR-IN-156
    		Inhibitor
    EGFR-IN-156 (Compound 7f) is an EGFR inhibitor that also has inhibitory activity against mutations EGFRL858R and EGFRT790M (IC50 values are 0.186, 0.131, and 0.107 μM, respectively). EGFR-IN-156 has significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer) (IC50 values are 1.67, 5.32, and 6.56 μM, respectively). EGFR-IN-156 inhibits cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. EGFR-IN-156 shows promise in EGFR-related cancers.
    EGFR-IN-156
  • HY-147862
    EGFR-IN-62
    		Inhibitor
    EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines.
    EGFR-IN-62
  • HY-178242
    PROTAC EGFR degrader 16
    		Degrader
    PROTAC EGFR degrader 16 (Compound 98) a selective EGFR PROTAC degrader with DC50 values of < 50 nM in NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R) and NCI-H1976 + CS (EGFR L858R-T970M-L797S). PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer (Pink: EGFR ligand (HY-178313); Blue: CRBN ligand (HY-W1128702); Black: Linker; EGFR ligand + Linker (HY-178311)).
    PROTAC EGFR degrader 16
  • HY-172471
    DSPE-PEG5000-GE11
    DSPE-PEG5000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG5000-GE11 can be used for drug delivery.
    DSPE-PEG5000-GE11
  • HY-179485
    EGFR/VEGFR2-IN-10
    		Inhibitor
    EGFR/VEGFR2-IN-10 is a selective EGFR, VEGFR2 and COX2 inhibitor with IC50s of 8.5, 68 and 158 nM, respectively. EGFR/VEGFR2-IN-10 induces G1-phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8, and elevates caspase-9 protein levels, confirming activation of the intrinsic apoptotic pathway. EGFR/VEGFR2-IN-10 demonstrates exceptional therapeutic potential by simultaneously inhibiting tumor proliferation, angiogenesis, and inflammation pathways while maintaining a favorable selectivity profile. EGFR/VEGFR2-IN-10 can be used as a research tool for cervical, liver, colon, and breast cancer studies.
    EGFR/VEGFR2-IN-10
  • HY-153605
    EGFR-IN-77
    		Inhibitor
    EGFR-IN-77 (Compound 4a) is a selective EGFRT790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFRT790M/L858R, 0.477 μM against EGFRL858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFRT790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFRL858R/T790M double-mutant non-small cell lung cancer.
    EGFR-IN-77
  • HY-180949
    EGFR-IN-189
    		Inhibitor
    EGFR-IN-189 (Compound 7) is a selective covalent epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 200 nM. EGFR-IN-189 can effectively inhibit the C797S mutant type of EGFR. EGFR-IN-189 can inhibit cancer cells proliferation and inhibit EGFR phosphorylation and downstream ERK1/2 phosphorylation. EGFR-IN-189 can be used for research of nonsmall cell lung cancer.
    EGFR-IN-189
  • HY-P991233
    BAT1006
    		Inhibitor
    BAT1006 is a monoclonal antibody targeting HER2 extracellular domain II with enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) for the study of HER2-positive locally advanced/metastatic solid tumors. BAT1006 has an approximately 5-fold enhanced ADCC effect compared to pertuzumab (HY-P9912) and exhibits potent anti-tumor activity in the HER2-positive Calu-3 xenograft mouse model.
    BAT1006
  • HY-178005
    EGFR-IN-174
    		Inhibitor
    EGFR-IN-174 is a potent EGFR inhibitor (IC50 = 0.17 μM) and also displays VEGFR-2 inhibition (IC50 = 0.2007 μM). EGFR-IN-174 exhibits potent anticancer effects with low cytotoxicity to normal cells. EGFR-IN-174 induces G2/M and Pre-G1 phase arrest and significantly triggers apoptosis. EGFR-IN-174 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer.
    EGFR-IN-174
  • HY-146472
    EGFR-IN-52
    		Inhibitor
    EGFR-IN-52 (Compound 4) is a potent EGFR inhibitor with IC50 values of 0.358, 86.02 and 432.67 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-52 shows cytotoxic activity against cancer cell lines and induces apoptosis.
    EGFR-IN-52
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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