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-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-175635
    EGFR/VEGFR2-IN-6
    		Inhibitor
    EGFR/VEGFR2-IN-6 (Compound 3k) is a dual-functional inhibitor of EGFR and VEGFR2 with IC50s of 10.53 and 3.37 μM for EGFR and VEGFR2, respectively. EGFR/VEGFR2-IN-6 has significant anti-proliferation activity against breast cancer cells, and induces G0/G1 cell cycle arrest and cell apoptosis, especially early apoptosis. EGFR/VEGFR2-IN-6 can be used for cancers research.
    EGFR/VEGFR2-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
  • HY-161045
    T-1-DOCA
    		Inhibitor
    T-1-DOCA ia a EGFR inhibitor, with the IC50 of 56.94 and 269.01?nM for EGFRWT and EGFRT790M, respectively. T-1-DOCA can induces cell apoptosis of HCT-116 cells.
    T-1-DOCA
  • HY-161320
    EGFR-IN-105
    		Inhibitor
    EGFR-IN-105 (Compound 5b) is an EGFR2 inhibitor with an IC50 value of 0.68 μM. EGFR-IN-105 exhibits anticancer activity and can induce apoptosis in cancer cells, which is used in the research of pancreatic cancer.
    EGFR-IN-105
  • HY-143445
    EGFR-IN-48
    		Inhibitor
    EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.
    EGFR-IN-48
  • HY-145867
    EGFR-IN-45
    		Inhibitor
    EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis.
    EGFR-IN-45
  • HY-160682
    EGFR/HER2-IN-12
    		Inhibitor
    EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant.
    EGFR/HER2-IN-12
  • HY-177710
    MEDI4276
    MEDI4276 is a biparatopic tetravalent antibody targeting two nonoverlapping epitopes in subdomains 2 and 4 of the HER2 ecto-domain. MEDI4276 is composed of MEDI4276 Antibody (HY-P991238) and a cytotoxic payload AZ1508 (HY-128962) linked through site-specific coupling. MEDI4276 exhibits antitumor activity.
    MEDI4276
  • HY-137028
    2′-Thioadenosine
    		Inhibitor
    2'-Thioadenosine (PD157432) is a selective and irreversible inhibitor of ErbB-1 and ErbB-2, with an IC50 of 45 µM for ErbB-2. 2'-Thioadenosine covalently inactivates ErbB-1 via modification of a cysteine residue at the active site.
    2′-Thioadenosine
  • HY-P991573
    Anti-EGFR Antibody (D2C7)
    		Inhibitor
    Anti-EGFR Antibody (D2C7) is a monoclonal antibody against EGFR. The recombinant immunotoxin D2C7-(scdsFv)-PE38KDEL constructed based on Anti-EGFR Antibody (D2C7) has antineoplastic activity in glioblastoma models.
    Anti-EGFR Antibody (D2C7)
  • HY-168151
    EGFR-IN-128
    		Inhibitor
    EGFR-IN-128 (compund 28) is a potent and selective molecule targeting wild-type EGFR Ex20Ins that demonstrates efficacy in multiple human xenograft models and can cross the blood-brain barrier in preclinical species.
    EGFR-IN-128
  • HY-168427
    Avitinib maleate dihydrate
    		Inhibitor
    Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects.
    Avitinib maleate dihydrate
  • HY-143901
    EGFR-IN-40
    		Inhibitor
    EGFR-IN-40 (compound 3z) is a potent BTK, EGFR, and ITK inhibitor with IC50 values of 1.2 nM, 5.3 nM, and 46.1 nM, respectively.
    EGFR-IN-40
  • HY-116504
    WB-308
    		Inhibitor
    WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
    WB-308
  • HY-161146
    EGFR-IN-100
    		Inhibitor
    EGFR-IN-100 (compound 3f) is a EGFR inhibitor with IC50 range of 0.137-0.507 μM. EGFR-IN-100 has antiproliferative activity and induces the apoptosis pathway. EGFR-IN-100 arrests the MCF-7 cell cycle at the S phase.
    EGFR-IN-100
  • HY-110039
    BIBX 1382 dihydrochloride
    		Inhibitor
    BIBX 1382 dihydrochloride is an ErbB kinase inhibitor with significant antiviral activity. BIBX 1382 affects the ability of viruses to enter host cells by inhibiting members of the ErbB kinase family. It can be used to study the interaction mechanism between virus and host and the broad spectrum intervention of highly pathogenic viruses.
    BIBX 1382 dihydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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