PF 543 hydrochloride

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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 (2)
Reviews

Biological Activity for PF 543 hydrochloride

PF 543 hydrochloride is a 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. Also reduces sickling, hemolysis and inflammation in a transgenic mouse model of sickle cell disease.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 543 hydrochloride

PF 543 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 543 hydrochloride

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PF 543 hydrochloride

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

Preparing Stock Solutions for PF 543 hydrochloride

The following data is based on the product molecular weight 502.07. Batch specific molecular weights may vary from batch to batch due to the degree 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

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Product Datasheets for PF 543 hydrochloride

References for PF 543 hydrochloride

References are publications that support the biological activity of the product.

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

Zhang et al (2014) Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression. J.Clin.Invest. 124 2750 PMID: 24837436


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2 Citations for PF 543 hydrochloride

Citations are publications that use Tocris products. Selected citations for PF 543 hydrochloride include:

Jiri et al (2021) A chemical screen for modulators of mRNA translation identifies a distinct mechanism of toxicity for sphingosine kinase inhibitors. PLoS Biol 19 e3001263 PMID: 34033645

Huilan et al (2021) aPC/PAR1 confers endothelial anti-apoptotic activity via a discrete, β-arrestin-2-mediated SphK1-S1PR1-Akt signaling axis. Proc Natl Acad Sci U S A 118 PMID: 34873055


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