PFK15

Catalog No.S7289 Synonyms: PFK-015

PFK15 Chemical Structure

Molecular Weight(MW): 260.29

PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.

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Biological Activity

Description PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
Targets
PFKFB3 [1]
207 nM
In vitro

PFK15 produces potent growth inhibition in a series of cancer cells. In Jurkat T-cell leukemia cells and H522 lung adenocarcinoma cells, PFK15 also reduces F26BP, glucose uptake, and intracellular ATP level. [1]

In vivo In vivo, PFK15 has adequate pharmacokinetic properties. PFK15 (25 mg/kg i.p.) suppresses the growth, metastatic spread, and glucose metabolism of LLC tumors in syngeneic mice. In three human xenograft models of cancer in athymic mice, PFK15 also yields antitumor effects that are comparable to approved chemotherapeutic agents. [1]

Protocol

Kinase Assay:

[1]

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Recombinant PFKFB3 assay:

Kinase reactions are conducted by incubating 13 ng of recombinant human PFKFB3 protein in a reaction mix containing 10 μmol/L ATP, 10 μmol/L F6P, and either dimethyl sulfoxide (DMSO) vehicle control, 3PO, or PFK15 for 1 hour at room temperature. Kinase activity is measured with the Adapta Universal Kinase Assay per manufacturer
Cell Research:

[1]

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  • Cell lines: 59 cancer cell lines
  • Concentrations: ~30 μM
  • Incubation Time: 48 hours
  • Method:

    Viability is determined using trypan blue exclusion. Cells were incubated in 20% trypan blue for 5 minutes. Cells excluding trypan blue are counted using a standard hemocytometer to determine the total number of viable cells. Experiments are conducted in triplicate.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: C57Bl/6 mice bearing LLC xenografts, Balb/C athymic mice bearing CT26, U-87 MG, or BxPC-3 xenografts.
  • Formulation: DMSO
  • Dosages: 25 mg/kg every 3 days
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 19 mg/mL warmed (72.99 mM)
Ethanol 2 mg/mL warmed (7.68 mM)
Water <1 mg/mL
In vivo 5% DMSO+45% PEG 300+1% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 260.29
Formula

C17 H12 N2 O

CAS No. 4382-63-2
Storage powder
in solvent
Synonyms PFK-015

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID