PF 543 hydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 5754
Potent and selective SphK1 inhibitor
Discontinued Product
5754 has been discontinued.
View all Sphingosine Kinase Inhibitors products.
Key Product Details
Description
Potent and selective SphK1 inhibitor
Product Description
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. Inhibits growth and metastasis of several types of cancer cell including ovarian, colorectal and breast cancers, and suppresses HCT-116 tumor xenograft growth in mice. Antifibrotic and anti-inflammatory in a range of in vivo disease models. 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.Product Specifications
Molecular Weight
502.07
Formula
C27H31NO4S.HCl
Storage
Desiccate at RT
Purity
≥98% (HPLC)
Chemical Name
(2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride
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.
Solubility
| 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 all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.99 mL | 9.96 mL | 19.92 mL |
| 5 mM | 0.40 mL | 1.99 mL | 3.98 mL |
| 10 mM | 0.20 mL | 1.00 mL | 1.99 mL |
| 50 mM | 0.04 mL | 0.20 mL | 0.40 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Yi Therapeutic potential of the sphingosine kinase 1 inhibitor, PF-543. Biomed.Pharmacother. 2023 PMID: 37167721
- Zhang Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression. J.Clin.Invest. 2014 PMID: 24837436
- Schnute Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem.J. 2012 PMID: 22397330
- Schnute Discovery of a potent and selective sphingosine kinase 1 inhibitor through the molecular combination of chemotype-distinct screening hits J.Med.Chem. 2017 PMID: 28231433
- Ju Targeting colorectal cancer cells by a novel sphingosine kinase 1 inhibitor PF-543. Biochem.Biophys.Res.Commun. 2016 PMID: 26775841
Product Specific Notices for PF 543 hydrochloride
For research use only
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