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-151573
    EGFR/CDK2-IN-1
    		Inhibitor
    EGFR/CDK2-IN-1 (Compound 3b) is an EGFR/CDK2 inhibitor. EGFR/CDK2-IN-1 shows good cytotoxicity against MCF7 and HepG2 cells. EGFR/CDK2-IN-1 can be used in cancer research.
    EGFR/CDK2-IN-1
  • HY-13314A
    Tesevatinib tosylate
    		Inhibitor
    Tesevatinib (XL-647) tosylate is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib tosylate significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib tosylate also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib tosylate can inhibit tumor proliferation and exhibits antitumor activity.
    Tesevatinib tosylate
  • HY-155200
    EGFR-IN-84
    		Inhibitor
    EGFR-IN-84 (Compound 6g) is an EGFR inhibitor (IC50: 24 nM). EGFR-IN-84 inhibits A549 cell growth (IC50: 1.537 μM). EGFR-IN-84 can be used for research of lung cancer.
    EGFR-IN-84
  • HY-170932
    EGFR/COX-2-IN-1
    		Inhibitor
    EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFRWT, EGFRT790M, COX-1 and COX-2 with IC50s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC50s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC50s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects.
    EGFR/COX-2-IN-1
  • HY-146239
    EGFR/HER2/TS-IN-2
    		Inhibitor
    EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC50 values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC50 of 1.69 µM.
    EGFR/HER2/TS-IN-2
  • HY-153856
    TAS2940
    		Inhibitor
    TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 can be used for the study of tumors with HER2 and EGFR aberrations.
    TAS2940
  • HY-170787
    TZEP7
    		Inhibitor
    TZEP7 is an EGFR kinase inhibitior in cancer cells. TZEP7 exhibits cytotoxic effects against cancer cell lines and induces apoptosis. TZEP7 demonstrates downregulation of antiapoptotic Bcl-2, upregulation of pro-apoptotic Bax, and increases caspase levels. TZEP7 is promising for research of anticancer agent.
    TZEP7
  • HY-P5258
    Oligopeptide-41
    		Inducer
    Oligopeptide-41 is a bioactive peptide with promotion of hair growth effect and has been reported used as a cosmetic ingredient.
    Oligopeptide-41
  • HY-162964
    EGFR-IN-126
    		Inhibitor
    EGFR-IN-126 (compound 9d) is a potent inhibitor of EGFRL858R/T790M/C797S, with the IC50 value of 0.005 μM. EGFR-IN-126 shows antitumor effects in vivo and in vitro.
    EGFR-IN-126
  • HY-147992
    EGFR/HER2-IN-4
    		Inhibitor
    EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research.
    EGFR/HER2-IN-4
  • HY-158176
    EGFR T790M/L858R-IN-5
    		Inhibitor
    EGFR T790M/L858R-IN-5 (example 52) is a potent inhibitor of EGFR T790M/L858R with the inhibition percentage of 92.9% in the concerntration of 0.05 μM.
    EGFR T790M/L858R-IN-5
  • HY-161067
    EGFR-IN-96
    		Inhibitor
    EGFR-IN-96 (compound 7a) is a thieno[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. EGFR-IN-96 arrests the growth of HepG2 cells in the S phase and G2/M phase, and inhibits the growth of cancer cells bearing EGFR wild-type and EGFRT790M.
    EGFR-IN-96
  • HY-157398
    EGFR T790M/L858R-IN-3
    		Inhibitor
    EGFR T790M/L858R-IN-3 (compound B1) is a EGFRL858R/T790M inhibitor with IC50 value of 13?nM. EGFR T790M/L858R-IN-3 shows anti-tumour activity in H1975 cells with an IC50 value of 0.087 μΜ. EGFR T790M/L858R-IN-3 inhibits cell migration in A549 cells and induces apoptosis in H1975 cells.
    EGFR T790M/L858R-IN-3
  • HY-145823
    EGFR-IN-42
    		Inhibitor
    EGFR-IN-42 (Compound 17b) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-42 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-42 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-42 has superior anti-cancer activity.
    EGFR-IN-42
  • HY-P10995
    TAT-327
    		Inhibitor
    TAT-327 is cell-penetrating peptide. TAT-327 selectively inserts into cancer cell membranes and shows potent antitumor activity. TAT-327 effectively inhibits cancer cells proliferation, induces apoptosis and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the Eps8/EGFR interaction. TAT-327 significantly inhibits tumor growth in HT-29 xenograft mcie models.
    TAT-327
  • HY-147997
    EGFR-IN-68
    		Inhibitor
    EGFR-IN-68 (Compound 8d) is a potent EGFR inhibitor with an IC50 of 0.33 μM. EGFR-IN-68 shows anticancer activity.
    EGFR-IN-68
  • HY-161891
    EGFR/Akt-IN-1
    		Inhibitor
    EGFR/Akt-IN-1 (compound 17) is a potent inhibitor of EGFR/Akt, with the IC50s of 12.89 μM and 10.88 μM in A549 cells, respectively. EGFR/Akt-IN-1 arrestes the cell cycle at the S phase.
    EGFR/Akt-IN-1
  • HY-167948
    Dacomitinib metabolite M1/2
    		Inhibitor
    Dacomitinib metabolite M1/2 is a potent inhibitor of both wild-type (WT) EGFR and the T790M mutation, demonstrating significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC).
    Dacomitinib metabolite M1/2
  • HY-146132
    EGFR-IN-55
    		Inhibitor
    EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC50 values of 70 nM and 3.9 nM against EGFRWT and EGFRL858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity.
    EGFR-IN-55
  • HY-172470
    DSPE-PEG2000-GE11
    DSPE-PEG2000-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-PEG2000-GE11 can be used for drug delivery.
    DSPE-PEG2000-GE11
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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