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-155079
    DZD1516
    98.31%
    DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models.
    DZD1516
  • HY-P990049
    Becotatug
    Inhibitor 98.44%
    Becotatug (JMT-101) is an IgG1 antibody targeting EGFR that can also be conjugated to Afatinib (HY-10261) and Osimertinib (HY-15772) as a synthetic ADC.
    Becotatug
  • HY-130616
    EGFR-IN-11
    Inhibitor 99.30%
    EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.
    EGFR-IN-11
  • HY-138627A
    AST5902 trimesylate
    Inhibitor 98.75%
    AST5902 trimesylate is the principal metabolite of Alflutinib (AST2818) both in vitro and in vivo. AST5902 trimesylate exerts antineoplastic activity. Alflutinib is an EGFR inhibitor.
    AST5902 trimesylate
  • HY-100214
    EAI001
    Inhibitor 99.88%
    EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer.
    EAI001
  • HY-10261S
    Afatinib-d6
    Inhibitor ≥99.0%
    Afatinib-d6 is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor[1].
    Afatinib-d<sub>6</sub>
  • HY-P99684
    Laprituximab
    Inhibitor
    Laprituximab (J2898A) is a humanized IgG1 anti-EGFR antibody that can be used for the synthesis of ADC IMGN289.
    Laprituximab
  • HY-108484
    PP 3
    Inhibitor 99.79%
    PP 3 (Compound 3) is an EGFR tyrosine kinase inhibitor with an IC50 of 2.7 μM.
    PP 3
  • HY-41404
    Piperonylic acid
    99.91%
    Piperonylic acid is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic Acid is a selective, mechanism-based inactivator of the trans-cinnamate 4-Hydroxylase. Piperonylic acid has anticancer, antioxidant and antibacterial activities.
    Piperonylic acid
  • HY-N6577
    Astragaloside VI
    99.95%
    Astragaloside VI could activate EGFR/ERK signalling pathway to improve wound healing.
    Astragaloside VI
  • HY-15729A
    Rociletinib hydrobromide
    Inhibitor 98.04%
    Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
    Rociletinib hydrobromide
  • HY-P99437
    Anbenitamab
    Inhibitor 99.22%
    Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting the extracellular domains II and IV of the human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathway. The IgG1 Fc fragment of Anbenitamab binds FcRγIIIa mediates potent antibody dependent cell-mediated cytotoxicity (ADCC) and inhibits tumor cell proliferation. Anbenitamab has the potential for HER2-positive metastatic breast cancer (MBC) research.
    Anbenitamab
  • HY-P99715
    Losatuxizumab
    Inhibitor
    Losatuxizumab (ABT-806) is an anti-EGFR monoclonal antibody. Losatuxizumab binds to EGFR with EC50s of 0.96 nM for EGFR wild-type, 0.09 nM for EGFRC271A,C283A, 0.12 nM for EGFRvIII, 0.66 nM for EGFR1-501. Losatuxizumab can be used for research of EGFR-expressing cancers.
    Losatuxizumab
  • HY-116437
    Selatinib
    Inhibitor 99.83%
    Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects.
    Selatinib
  • HY-112345
    PD-089828
    Inhibitor 98.07%
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
    PD-089828
  • HY-N2184
    Furanodienone
    99.90%
    Furanodienone is one of the major bioactive constituents derived from Rhizoma Curcumae. Furanodienone induced apoptosis.
    Furanodienone
  • HY-P99866
    Duligotuzumab
    Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody that specifically targets Her3 (ErbB3).
    Duligotuzumab
  • HY-132259
    Depatuxizumab mafodotin
    Depatuxizumab mafodotin is an antibody-drug conjugate (ADC) that specifically targets the epidermal growth factor receptor (EGFR). Depatuxizumab mafodotin can be used for cancer research.
    Depatuxizumab mafodotin
  • HY-10531
    ARRY-380 analog
    Inhibitor 99.19%
    ARRY-380 analog, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2.
    ARRY-380 analog
  • HY-101426
    RG14620
    Inhibitor 98.09%
    RG14620 is an EGFR inhibitor with an IC50 of 3 μM.
    RG14620
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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