1. Signaling Pathways
  2. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  3. EGFR

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P99455
    Bafisontamab
    Inhibitor 99.9%
    Bafisontamab (EMB-01) is a bispecific antibody targeting EGFR and cMET with antitumor activity.
    Bafisontamab
  • HY-108016
    Peruvoside
    Inhibitor 99.32%
    Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib.
    Peruvoside
  • HY-112097
    E260
    Inhibitor 99.92%
    E260 is a Fer/FerT kinase inhibitor.
    E260
  • HY-109061B
    Lazertinib mesylate
    Inhibitor 99.85%
    Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.
    Lazertinib mesylate
  • HY-13464
    ALK-IN-1
    Inhibitor 99.94%
    ALK-IN-1 is an orally active, blood-brain barrier-permeable ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer.
    ALK-IN-1
  • HY-12026
    WZ4002
    Inhibitor 98.99%
    WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFRL858R, EGFRL858R/T790M, EGFRE746_A750 and EGFRE746_A750/T790M, respectively.
    WZ4002
  • HY-137191
    CH7233163
    Inhibitor 99.41%
    CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities.
    CH7233163
  • HY-P990071
    Fepixnebart
    Inhibitor
    Fepixnebart (LY3016859) is a humanized monoclonal hIgG4 antibody, which binds and neutralizes only TGFα and epiregulin with high affinity. Fepixnebart can be used for the study of diabetic nephropathy and broad-spectrum chronic pain, including diabetic peripheral neuropathic pain (DPNP), signs and symptoms of osteoarthritis (OA), and chronic low back pain (CLBP).
    Fepixnebart
  • HY-P99684
    Laprituximab
    Inhibitor 99.74%
    Laprituximab (J2898A) is a humanized IgG1 anti-EGFR antibody that can be used for the synthesis of ADC IMGN289.
    Laprituximab
  • HY-15844
    AG-825
    Inhibitor 98.13%
    AG-825 is a selective, ATP-competitive, tyrosine phosphorylation ErbB2 inhibitor with an IC50 of 0.35 μM. AG825 significantly accelerates Apoptosis of human neutrophils. AG-825 increases β1AR density. AAG-825 has anticancer and anti-inflammatory activities. AAG-825 can be used in cardiovascular disease research.
    AG-825
  • HY-115481
    EphB1-IN-1
    Inhibitor 99.51%
    EphB1-IN-1 (Compound 1) is a potent EphB1 inhibitor with IC50s of 3.0, 15 and 220 nM against EphB1G703C, EphB1T697G and EphB1WT, respectively.
    EphB1-IN-1
  • HY-B0794
    AZ7550
    Inhibitor
    AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
    AZ7550
  • HY-147858
    PROTAC EGFR degrader 7
    Inhibitor 99.48%
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research. PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC EGFR degrader 7
  • HY-P990238
    Anti-Human/Rat HER2 (neu) Antibody (7.16.4)
    Inhibitor
    Anti-Human/Rat HER2 (neu) Antibody (7.16.4) is an anti-human and anti-rat HER2 IgG2a monoclonal antibody. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) reduces tumor cell proliferation by inhibiting the HER2 signaling pathway. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) can activate CD8+ T cells. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) can be used for research on cancer such as breast cancer.
    Anti-Human/Rat HER2 (neu) Antibody (7.16.4)
  • HY-19729
    Naquotinib
    Inhibitor 98.10%
    Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
    Naquotinib
  • HY-19803
    Naquotinib mesylate
    Inhibitor 98.06%
    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
    Naquotinib mesylate
  • HY-19816A
    Avitinib maleate
    Inhibitor 99.86%
    Avitinib (Abivertinib) maleate 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 is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects.
    Avitinib maleate
  • HY-12972
    Mavelertinib
    Inhibitor 99.34%
    Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
    Mavelertinib
  • HY-107364
    MTX-211
    Inhibitor 99.81%
    MTX-211 (Mol 211) is a dual inhibitor of EGFR and PI3K with IC50 values of <100 nM. MTX-211 can be used for the research of cancer and other diseases.
    MTX-211
  • HY-13314
    Tesevatinib
    Inhibitor 99.41%
    Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity.
    Tesevatinib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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