PF 543 hydrochloride
Tocris Bioscience | Catalog # 5754
Key Product Details
Description
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 for PF 543 hydrochloride
Molecular Weight
Formula
Storage
Purity
Chemical Name
CAS Number
PubChem ID
InChI Key
SMILES
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
Background References
References are publications that support the biological activity of the product. See our Citations tab to view 4 publications citing the usage of this 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 Documents for PF 543 hydrochloride
Certificate of Analysis
To download a Certificate of Analysis, please enter a lot or batch number in the search box below.
Product Specific Notices for PF 543 hydrochloride
For research use only
Related Research Areas
Citations for PF 543 hydrochloride
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