1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Anti-infection
  2. EGFR
    HCV
    Influenza Virus
  3. AG-1478 hydrochloride

AG-1478 hydrochloride (Synonyms: Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride)

Cat. No.: HY-13524A
Handling Instructions

AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV).

For research use only. We do not sell to patients.

AG-1478 hydrochloride Chemical Structure

AG-1478 hydrochloride Chemical Structure

CAS No. : 170449-18-0

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Top Publications Citing Use of Products

    AG-1478 hydrochloride purchased from MCE. Usage Cited in: Sci Rep. 2017 Jan 19;7:40802.

    EGFR participates the process of ACh induced cell proliferation and signaling transduction. After adding 10 μM EGFR specific inhibitor AG1478 2 h prior to ACh addition, protein changes are analyzed by western blot.
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    Description

    AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV)[1][2][3][4].

    IC50 & Target[1][4]

    EGFR

    3 nM (IC50)

    HCV

     

    EMCV

     

    In Vitro

    AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC50 of 4 nM[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells[3].

    In Vivo

    Administration of AG-1478 (AG1478) significantly reduces myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. ApoE-/- mice are first fed with HFD for 8 weeks (ApoE-HFD), and then administrated with AG-1478 (10 mg/kg/day) or 542 (10 mg/kg/day) for another 8 weeks by oral gavage. AG-1478 or 542 treatment blocks HFD induced cardiac EGFR phosphorylation in vivo, without affecting the plasma level of low density lipoprotein (LDL) and total triglyceride (TG)[2]. Administration of EGF (10 nM) leads to a robust and reproducible elevation in EGFR phosphorylation that can be blocked by AG-1478 (AG1478), a known inhibitor of EGFR phosphorylation. Increasing doses of Polyfect (PF) result in a significant reduction in EGF-induced EGFR phosphorylation (p<0.05) but this is to a lesser extent than observed with AG1478[3].

    Molecular Weight

    352.22

    Formula

    C₁₆H₁₅Cl₂N₃O₂

    CAS No.

    170449-18-0

    SMILES

    COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

    AG-1478Tyrphostin AG-1478NSC 693255AG1478AG 1478Tyrphostin AG1478Tyrphostin AG 1478NSC693255NSC-693255EGFRHCVInfluenza VirusEpidermal growth factor receptorErbB-1HER1Hepatitis C virusantiviralencephalomyocarditisvirusEMCVobesitymyocardialinjurycardiovasculardiseasescancerchemotherapyInhibitorinhibitorinhibit

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