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GW-2580

cFMS Receptor Tyrosine Kinase Inhibitor

An Inhibitor of Trk Receptors and cFMS/CSF-1 Receptor Kinases 

Cat #: G-255
Alternative Name cFMS Receptor Tyrosine Kinase Inhibitor
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 366.41
    Purity: >99%
    Effective concentration 1-100 µM.
    Structure
    Chemical name 5-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine.
    Molecular formula C20H22N4O3.
    CAS No.: 870483-87-7
    PubChem CID 11617559
    Activity GW-2580 is a potent and selective inhibitor of cFMS/CSF-1 receptor kinase, shown to completely and selectively inhibit human cFMS kinase activity at 60 nM, and fully suppress CSF-1 induced cell growth at 1 μM, in vitro. Orally bioavailable and active in vivo1. GW 2580 also binds to TrkB, TrkC and TrkA with Kd values of 36 nM, 120 nM and 630 nM, respectively,2 and fully inhibits BDNF-induced TrkB phosphorylation in cells at 3 µM3.
    References-Activity
    1. Conway, J.G. et al. (2005) Proc. Natl. Acad. Sci. U. S. A. 102, 16078.
    2. Karaman, M.W. et al. (2008) Nat. Biotechnol. 26, 127.
    3. Cohen, M.S. et al. (2011) Proc. Natl. Acad. Sci. U. S. A. 108, 11246.
    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 up to 100mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Store at -20°C.
    Our bioassay
    • Alomone Labs GW-2580 inhibits BDNF-induced phosphorylation of ERK1/2 in TrkB-expressing HEK-293 cells.
      Alomone Labs GW-2580 inhibits BDNF-induced phosphorylation of ERK1/2 in TrkB-expressing HEK-293 cells.
      Serum-deprived cells were stimulated with 10 ng/ml Recombinant human BDNF protein (#B-250) following pre-incubation with control, 1 µM, 10 µM and 100 µM GW-2580 (#G-255). Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-ERK1/2.
    • Alomone Labs GW-2580 inhibits NGF-mediated survival of serum-deprived PC12 cells.
      Alomone Labs GW-2580 inhibits NGF-mediated survival of serum-deprived PC12 cells.
      Dose-response curve of GW-2580 (#G-255) inhibition of 50 ng/ml Recombinant human beta-NGF protein (#N-245) mediated survival of serum-deprived PC12 cells. Cell viability was determined by the XTT method and normalized to control. IC50 was calculated at 2.88 µM.
    References - Scientific background
    1. Conway, J.G. et al. (2005) Proc. Natl. Acad. Sci. U. S. A. 102, 16078.
    2. Karaman, M.W. et al. (2008) Nat. Biotechnol. 26, 127.
    3. Cohen, M.S. et al. (2011) Proc. Natl. Acad. Sci. U. S. A. 108, 11246.
    Scientific background

    GW-2580 is a small-molecule pyrimidine derivative, that acts as a potent and selective inhibitor of Colony-stimulating factor 1 (CSF-1) signaling through cFMS kinase receptor. GW-2580 completely inhibits human cFMS kinase in vitro at 0.06 μM1. 

    The compound also acts as an inhibitor of Trk Receptors and shows binding towards TrkB, TrkC, and TrkA with Kd values of 36 nM, 120 nM and 630 nM, respectively2 and fully inhibits BDNF-induced TrkB phosphorylation in cells at 3 µM3.

    Target CSF-1R receptor, Trk receptor
    Lyophilized Powder
    Last update: 02/01/2022

    GW-2580 (#G-255) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
    Shipping and Ordering information

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