PF 543 hydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 5754 - PF 543 hydrochloride | C27H31NO4S.HCl | CAS No. 1706522-79-3
Description: Potent and selective SphK1 inhibitor
Chemical Name: (2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 502.07
Formula C27H31NO4S.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1706522-79-3
PubChem ID 121230770
InChI Key WNKWAZFYPZMDGJ-VQIWEWKSSA-N
Smiles CC1=CC(OCC2=CC=C(CN3CCC[C@@H]3CO)C=C2)=CC(CS(C4=CC=CC=C4)(=O)=O)=C1.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.21 100
ethanol 10.04 20
water 5.02 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 502.07. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.99 mL 9.96 mL 19.92 mL
5 mM 0.4 mL 1.99 mL 3.98 mL
10 mM 0.2 mL 1 mL 1.99 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Ju et al (2016) Targeting colorectal cancer cells by a novel sphingosine kinase 1 inhibitor PF-543. Biochem.Biophys.Res.Commun. 470 728 PMID: 26775841

Schnute et al (2012) Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem.J. 444 79 PMID: 22397330

Schnute et al (2017) Discovery of a potent and selective sphingosine kinase 1 inhibitor through the molecular combination of chemotype-distinct screening hits J.Med.Chem. 60 2562 PMID: 28231433


If you know of a relevant reference for PF 543 hydrochloride, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Sphingosine Kinase Inhibitors

Keywords: PF543 hydrochloride potent selective sphingosine kinases Sphk1 inhibitors inhibits Sphingosine Kinase

Citations for PF 543 hydrochloride

Citations are publications that use Tocris products.

Currently there are no citations for PF 543 hydrochloride. Do you know of a great paper that uses PF 543 hydrochloride from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for PF 543 hydrochloride

Protocols

TODO: Add Protocols