Biological Activity
Originally reported to be a selective PFKFB3 inhibitor (IC50 = 207 nM); a more recent report failed to demonstrate activity in a PFKFB3 kinase assay. Selective for PFKFB3 over a panel of 96 kinases. Reduces glucose uptake and induces apoptosis in H522 lung adenocarcinoma and Jurkat T cell leukemia cells. Suppresses glucose uptake and tumor growth, and inhibits metastasis of Lewis lung carcinoma cell xenografts in mice.
Technical Data
| M. Wt | 260.29 |
| Formula | C17H12N2O |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 4382-63-2 |
| PubChem ID | 25142799 |
| InChI Key | UJJUKZPBUMCSJZ-BQYQJAHWSA-N |
| Smiles | O=C(/C=C/C2=CC=C(C=CC=C3)C3=N2)C1=CC=NC=C1 |
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 | 26.03 | 100 | |
| ethanol | 2.6 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 260.29. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.84 mL | 19.21 mL | 38.42 mL |
| 5 mM | 0.77 mL | 3.84 mL | 7.68 mL |
| 10 mM | 0.38 mL | 1.92 mL | 3.84 mL |
| 50 mM | 0.08 mL | 0.38 mL | 0.77 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Clem et al (2013) Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer. Mol.Cancer Ther. 12 1461 PMID: 23674815
Brooke et al (2014) Targeting the Warburg effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). Bioorg.Med.Chem. 22 1029 PMID: 24398380
Keywords: PFK 15, supplier, PFK15, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase, selective, PFKFB3, inhibitors, inhibits, antitumor, PFKFB3, PFKFB3, Tocris Bioscience
