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PF-06439015

A Potent Inhibitor of TrkA/B and other Receptor Tyrosine Kinases

Cat #: P-355
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 407.52
    Purity: >99% (HPLC)
    Effective concentration 1-100 nM.
    Structure
    Chemical name (2R)-2-[5-[6-amino-5-[(1R)-1-[5-fluoro-2-(triazol-2-yl)phenyl]ethoxy]pyridin-3-yl]-4-methyl-1,3-thiazol-2-yl]propane-1,2-diol.
    Molecular formula C22H23FN6O3S.
    PubChem CID 72710568
    Activity PF-06439015 is a novel potent inhibitor of receptor tyrosine kinases, highly effective against crizotinib-resistant ALK mutants, inhibiting wild-type and mutant ALK phosphorylation with IC50 of 0.8 nM and 0.2 nM-24 nM, respectively. It is shown to inhibit kinase activity of ROS1, FER, LTK and TrkB with IC50 values of under 10 nM1.
    References-Activity
    1. Huang, Q. et al. (2014) J. Med. Chem. 57, 1170.
    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 before reconstitution (10000 x g 5 min).
    Storage of solutions Store at -20°C.
    Our bioassay
    • Alomone Labs PF-06439015 inhibits BDNF-induced ERK1/2 (p42/44 MAPK) phosphorylation in TrkB-expressing HEK 293 cells.
      Alomone Labs PF-06439015 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, 8 nM, 80 nM and 800 nM PF-06439015 (#P-355). Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-ERK1/2.
    • Alomone Labs PF-06439015 inhibits NGF-mediated survival of serum-deprived PC12 cells.
      Alomone Labs PF-06439015 inhibits NGF-mediated survival of serum-deprived PC12 cells.
      Dose-response curve of PF-06439015 (#P-355) inhibition of the 50 ng/ml 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 135.6 nM.
    References - Scientific background
    1. Huang, Q. et al. (2014) J. Med. Chem. 57, 1170.
    2. Paul, M.K. and Mukhopadhyay, A.K. (2004) Int. J. Med. Sci. 1, 101.
    Scientific background

    PF-06439015 is a synthetic compound that acts as a potent inhibitor of receptor tyrosine kinases. It inhibits various tyrosine kinases including ALK, ROS1, FER, LTK and TrkB with IC50 values of less than 10 nM1.

    Tyrosine kinases are a family of enzymes that acts as important mediators of the signaling cascade leading to cell proliferation, differentiation, migration, metabolism, and programmed cell death. Tyrosine kinases catalyze phosphorylation of select tyrosine residues in target proteins2.

    Target ALK, ROS1, FER, LTK and TrkA/B receptors
    Last update: 11/04/2021

    PF-06439015 (#P-355) is a highly pure, synthetic, and biologically active compound.

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