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-168073
    EGFR/VEGFR2-IN-1
    		Inhibitor
    EGFR/VEGFR2-IN-1 (Compound 10e) is a VEGFR-2 and EGFR inhibitor (IC50: 0.26 and 0.14 μM respectively). EGFR/VEGFR2-IN-1 inhibits tubulin polymerization with an IC50 of 40.9 μM. EGFR/VEGFR2-IN-1 induces apoptosis. EGFR/VEGFR2-IN-1 can be used for research of antileukemia and antilymphoma.
    EGFR/VEGFR2-IN-1
  • HY-10261E
    (R)-Afatinib
    		Inhibitor
    (R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) 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 can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    (R)-Afatinib
  • HY-159519
    EGFR/HER2-IN-16
    		Inhibitor
    EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research.
    EGFR/HER2-IN-16
  • HY-146238
    EGFR/HER2/TS-IN-1
    		Inhibitor
    EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC50 values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis.
    EGFR/HER2/TS-IN-1
  • HY-149632
    EGFR/HER2/DHFR-IN-2
    		Inhibitor
    EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth.
    EGFR/HER2/DHFR-IN-2
  • HY-164399
    SST0116CL1
    		Degrader
    SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth.
    SST0116CL1
  • HY-172469
    DSPE-PEG1000-GE11
    DSPE-PEG1000-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-PEG1000-GE11 can be used for drug delivery.
    DSPE-PEG1000-GE11
  • HY-170968
    EGFR-IN-150
    		Inhibitor
    EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer.
    EGFR-IN-150
  • HY-149401
    EGFR-IN-82
    		Inhibitor
    EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFRWT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
    EGFR-IN-82
  • HY-113549
    Erbstatin
    		Inhibitor
    Erbstatin, a EGFR kinase inhibitor, possesses antineoplastic effect.
    Erbstatin
  • HY-173146
    EGFR-IN-153
    		Inhibitor
    EGFR-IN-153 (Compound 5l) is an EGFR inhibitor. EGFR-IN-153 can inhibit the proliferation (IC50: 0.73 μM) and induce apoptosis of MDA-MB-231 cell. EGFR-IN-153 can be used for the research of breast cancer.
    EGFR-IN-153
  • HY-174841
    EGFR/HER2-IN-19
    		Inhibitor
    EGFR/HER2-IN-19 (Compound L1) is a dual inhibitor against epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). EGFR/HER2-IN-19 is promising for research of cancers driven by EGFR/HER2.
    EGFR/HER2-IN-19
  • HY-RS04210
    Egfr Mouse Pre-designed siRNA Set A
    		Inhibitor

    Egfr Mouse Pre-designed siRNA Set A contains three designed siRNAs for Egfr gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Egfr Mouse Pre-designed siRNA Set A
  • HY-P5742A
    ELAAWCRWGFLLALLPPGIAG TFA
    ELAAWCRWGFLLALLPPGIAG TFA (P5) is derived from rat HER2/neu protein with 21 amino acid length (aa 5-25). ELAAWCRWGFLLALLPPGIAG TFA can induce cytotoxic T lymphocyte (CTL) responses in mice bearing HER2-positive tumours.
    ELAAWCRWGFLLALLPPGIAG TFA
  • HY-135216
    Antiproliferative agent-54
    		Inhibitor
    Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC50 of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC50 of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats.
    Antiproliferative agent-54
  • HY-153557A
    HER2-IN-14
    		Inhibitor
    HER2-IN-14 (Compound 34) is an HER2 inhibitor with an IC50 of 18 nM. HER2-IN-14 also inhibits wt-EGFR with an IC50 of 6.3 μM.
    HER2-IN-14
  • HY-156470
    Multi-kinase-IN-6
    		Inhibitor
    Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
    Multi-kinase-IN-6
  • HY-107450
    PROTAC Her3-binding moiety 2
    		Inhibitor
    PROTAC Her3-binding moiety 2 is a Her3 inhibitor. PROTAC Her3-binding moiety 2 can be used for synthesis of PROTAC Her3 Degrader-8 (HY-153796).
    PROTAC Her3-binding moiety 2
  • HY-139884
    EGFR-IN-18
    		Inhibitor
    EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM).
    EGFR-IN-18
  • HY-W174279
    Tyrphostin 8
    		Inhibitor ≥98.0%
    Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM).
    Tyrphostin 8
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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