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AZD-1332

AZ-23 racemate, AZ-23 compound, 5-Chloro-2-N-[1-(5-fluoropyridin-2-yl)ethyl]-4-N-(3-propan-2-yloxy-1H-pyrazol-5-yl)pyrimidine-2,4-diamine

A Potent and Selective Inhibitor of TrkA, TrkB, TrkC Receptors

Cat #: A-495
Alternative Name AZ-23 racemate, AZ-23 compound, 5-Chloro-2-N-[1-(5-fluoropyridin-2-yl)ethyl]-4-N-(3-propan-2-yloxy-1H-pyrazol-5-yl)pyrimidine-2,4-diamine
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 391.8
    Purity: >95%
    Effective concentration 1-100 nM.
    Structure
    Chemical name 5-chloro-2-N-[1-(5-fluoropyridin-2-yl)ethyl]-4-N-(3-propan-2-yloxy-1H-pyrazol-5-yl)pyrimidine-2,4-diamine.
    Molecular formula C17H19ClFN7O.
    PubChem CID 49831044
    Activity AZD-1332 is a potent, selective, and orally bioavailable inhibitor of tyrosine kinase receptors (IC50 values of <10nM for TrkA and TrkB)1.
    References-Activity
    1. Thress, K. et al. (2009) Mol. Cancer. Ther. 8, 1818.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    • Alomone Labs AZD-1332 inhibits NGF-mediated survival of serum-deprived PC12 cells.
      Alomone Labs AZD-1332 inhibits NGF-mediated survival of serum-deprived PC12 cells.
      Dose-response curve of AZD-1332 (#A-495) inhibition of Native mouse NGF 2.5S protein (>95%) (#N-100) mediated survival of serum-deprived PC12 cells. Cell viability was determined by the XTT method and normalized to control. IC50 was calculated at 1.9 nM.
    • Alomone Labs AZD-1332 inhibits BDNF-induced ERK1/2 (p42/44 MAPK) phosphorylation in TrkB-expressing HEK 293 cells.
      Alomone Labs AZD-1332 inhibits BDNF-induced ERK1/2 (p42/44 MAPK) phosphorylation in TrkB-expressing HEK 293 cells.
      Serum-deprived cells were stimulated with 10 ng/ml Recombinant human BDNF protein (#B-250) in the presence of 0 nM, 5 nM, 50 nM and 500 nM AZD-1332 (#A-495). Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-ERK1/2. Complete inhibition of signal is achieved at 50 nM.
    References - Scientific background
    1. Thress, K. et al. (2009) Mol. Cancer. Ther. 8, 1818.
    2. Wang, T. et al. (2008) J. Med. Chem. 51, 4672.
    Scientific background

    AZD-1332 is a potent and selective inhibitor of the Tropomyosin-related kinase (TrkA, TrkB, and TrkC) receptors. The compound is at least 30-fold more specific towards Trk in cell-based assays over a wide range of other kinases tested. AZD-1332 inhibits Trk kinase activity in cells at low nanomolar concentrations, the compound demonstrates IC50 values of <10 nM for TrkA and TrkB1.

    TrkA, TrkB, and TrkC receptors are involved in neuronal cell growth, development, and survival. Trk receptors are also potent oncogenes involved in malignant transformation, metastasis, and survival signaling in human tumors1,2.

    Target TrkA, TrkB, TrkC receptors
    Lyophilized Powder
    Last update: 11/04/2021

    AZD-1332 (#A-495) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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