PFK 15

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Cat.No. 5339 - PFK 15 | C17H12N2O | CAS No. 4382-63-2
Description: Selective PFKFB3 inhibitor
Chemical Name: 1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

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

Safety Datasheet

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: 4398380


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Keywords: PFK 15, supplier, PFK15, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase, selective, PFKFB3, inhibitors, inhibits, antitumor, PFKFB3, PFKFB3, Tocris Bioscience

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