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-P99041
    Panitumumab
    Inhibitor 99.77%
    Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab can be used in the research of cancers, such as colon cancer.
    Panitumumab
  • HY-P9907A
    Trastuzumab (anti-HER2)
    Inhibitor 99.838%
    Trastuzumab (anti-HER2) is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab (anti-HER2) has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
    Trastuzumab (anti-HER2)
  • HY-P99380
    Zanidatamab
    Inhibitor 98.56%
    Zanidatamab (ZW25) is a humanised, bispecific monoclonal antibody targeting 2 distinct HER2 epitopes (ECD2 and ECD4). Zanidatamab has anti-tumour activity.
    Zanidatamab
  • HY-13272
    Dacomitinib
    Inhibitor 99.74%
    Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
    Dacomitinib
  • HY-13524
    AG-1478
    Inhibitor 99.57%
    AG-1478 (Tyrphostin AG-1478) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 has antiviral effects against HCV and encephalomyocarditis virus (EMCV).
    AG-1478
  • HY-P0221
    PACAP (1-38), human, ovine, rat
    Inducer 99.99%
    PACAP (1-38), human, ovine, rat is a PAC1 receptor agonist. PACAP (1-38), human, ovine, rat binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC50s of 4 nM, 2 nM, and 1 nM, respectively. PACAP (1-38), human, ovine, rat increases the α-secretase activity. PACAP (1-38), human, ovine, rat elevates cytosolic Ca2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP (1-38), human, ovine, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP (1-38), human, ovine, rat can be used for neurotrophic and neuroprotective research.
    PACAP (1-38), human, ovine, rat
  • HY-P99275
    Patritumab
    Inhibitor 99.28%
    Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors.
    Patritumab
  • HY-15772A
    Osimertinib mesylate
    Inhibitor 99.97%
    Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
    Osimertinib mesylate
  • HY-109061
    Lazertinib
    Inhibitor 99.87%
    Lazertinib (YH25448; GNS-1480) 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 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 induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib 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 is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.
    Lazertinib
  • HY-P10408
    Candidalysin
    Activator 99.81%
    Candidalysin is a cytolytic peptide toxin secreted by the fungus Candida albicans. Candidalysin drives epithelial immune responses by activating the EGFR-MAPK signaling pathway, inducing MMP expression and calcium influx, and regulating the c-Fos transcription factor and MKP1 via p38 MAPK and ERK1/2 respectively. Candidalysin is essential for mucosal and systemic infections, activating NLRP3 to promote inflammatory responses, neutrophil recruitment, and Th17 immunity. Candidalysin activates LDH causing membrane damage and exhibiting cytotoxicity
    Candidalysin
  • HY-P9921A
    Trastuzumab emtansine (solution)
    98.27%
    Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine), and the drug-linker conjugate for ADC is SMCC-DM1 (HY-101070). Trastuzumab emtansine can be used for the research of advanced breast cancer.
    Trastuzumab emtansine (solution)
  • HY-101084
    NSC 228155
    Activator
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
    NSC 228155
  • HY-P99406
    Petosemtamab
    Degrader 99.94%
    Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC).
    Petosemtamab
  • HY-164992
    Trastuzumab vedotin
    Inhibitor
    Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma.
    Trastuzumab vedotin
  • HY-P99507
    Zenocutuzumab
    Inhibitor 99.9%
    Zenocutuzumab (MCLA-128) is a bispecific humanized IgG1 antibody containing two different Fab arms, targeting extracellular domains of HER2 and HER3.
    Zenocutuzumab
  • HY-164702
    BL-B01D1
    Inhibitor 99.65%
    BL-B01D1 is a bispecific ADC, which targets EGFR and HER3 through bispecific antibody Izalontamab (HY-P99676), and exhibits cytotoxicity against various cancer cells via inhibition of DNA replication and DNA synthesis by its ADC toxin ED04 (HY-153891). BL-B01D1 can be used in the study of cancer.
    BL-B01D1
  • HY-12008
    Erlotinib Hydrochloride
    Inhibitor 99.94%
    Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib Hydrochloride
  • HY-10261A
    Afatinib dimaleate
    Inhibitor 99.74%
    Afatinib (BIBW 2992) dimaleate 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 dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib dimaleate
  • HY-13595
    Chrysophanol
    Inhibitor 99.73%
    Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
    Chrysophanol
  • HY-13050
    Sapitinib
    Inhibitor 99.93%
    Sapitinib (AZD-8931) 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
Cat. No. Product Name / Synonyms Species Source
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