PF 543 hydrochloride

Cat. No. 5754

PF 543 hydrochloride C27H31NO4S.HCl [1706522-79-3]

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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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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.

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Keywords: PF 543 hydrochloride, supplier, PF543, hydrochloride, potent, selective, sphingosine, kinases, Sphk1, inhibitors, inhibits, Tocris Bioscience, Sphingosine Kinase Inhibitor products

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