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:
    502.07
  • Formula:
    C27H31NO4S.HCl
  • Solubility:
    Soluble to 10 mM in water with gentle warming and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    1706522-79-3
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
  3. Discovery of a potent and selective sphingosine kinase 1 inhibitor through the molecular combination of chemotype-distinct screening hits
    Schnute et al.
    J.Med.Chem., 2017;60:2562

Have you used PF 543 hydrochloride?

Submit a review and receive a $25US/€18/£15/$25CAN amazon gift card if you include an image - $10US/€7/£6/$10CAN Amazon card for reviews without an image. Limited to verified customers in USA, Canada and Europe.

Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details

Note:

Contact Information

Calculators

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

R&D Systems Guarantee

Feedback

Customer Information