Catalog Number: 5754
Chemical Name: (2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride
Biological Activity
Potent and selective SphK1 inhibitor (IC50 = 2 nM; Ki = 3.6 nM). Exhibits >100-fold selectivity for Sphk1 over Sphk2. Also exhibits >5,000 fold selectivity over S1P1-5 receptors and 48 protein and lipid kinases. Attenuates proliferation and induces necrosis in human colorectal cancer cells in vitro. Suppresses HCT-116 tumor xenograft growth in mice.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 10 mM in water with gentle warming and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1.
    Schnute et al.
    Biochem.J., 2012;444:79
  2. Targeting colorectal cancer cells by a novel sphingosine kinase 1 inhibitor PF-543.
    Ju et al.
    Biochem.Biophys.Res.Commun., 2016;470:728
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