For research use only.

Catalog No.S7289 Synonyms: PFK-015

12 publications

PFK15 Chemical Structure

CAS No. 4382-63-2

PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.

Selleck's PFK15 has been cited by 12 publications

3 Customer Reviews

  • b EdU incorporation assays indicated PFK15 inhibited the cell proliferation of Cal27 cells. c The quantitative data of the EdU incorporation assays.

    J Exp Clin Cancer Res, 2017, 36(1):7. PFK15 purchased from Selleck.

    RA FLSs were pretreated with DMSO (as the control) or various concentrations of a specific PFKFB3 inhibitor, PFK15, for 4 h (A). The expression of IL-6, IL-8, CCL-2 and CXCL-10 was measured by real-time qPCR. The data are representative of independent experiments (means ± SEM) from10 RA patients. *P < 0.05, significantly different from control or SiC; #P < 0.05, significantly different from treatment with TNF-α alone

    Br J Pharmacol, 2017, 174(9):893-908. PFK15 purchased from Selleck.

  • (a, b) Cells were treated with the indicated concentrations of PFK15 for 12 h in the upper chambers and the lower chambers were filled with 10% FBS medium. Then, the invaded cells were stained with crystal violet and observed under a microscope with 200× magnification. Data were obtained from six randomly chosen fields and were normalized to the control group. (c) Proteins related with cell migration and invasion were detected. Phospho-FAK levels were downregulated in 7 and 9 μM while phospho-Cadherin E levels upregulated in both cell lines. Columns, mean; bars, SD. *P<0.05, compared with controls.

    PLoS One, 2016, 11(9):e0163768. PFK15 purchased from Selleck.

Purity & Quality Control

Choose Selective PFKFB Inhibitors

Biological Activity

Description PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
PFKFB3 [1]
(Cell-free assay)
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]

Methods Test Index PMID
Western blot
Cyclin E1 / CDK2 / Cyclin D1 / CDK4 / CDK6 / E2F1 / Rb / p-Rb ; 

PubMed: 27669567     

Cells were treated with various concentration of PFK15 for 24 h. The cell cycle associated proteins were checked by western bolt assay. PFK15 treatment significantly decreased expressions of cyclin D1, cyclin E1, phosphorylated Rb and the nuclear transfactor E2F-1 levels while increased non-phosphorylated Rb protein levels in both MKN45 and AGS cell lines.

Growth inhibition assay
Cell viability; 

PubMed: 27669567     

Cells grown in exponential phase were exposed to the indicated concentrations of PFK15 and, after 24 h, the effects on viability were determined by trypan blue exclusion. *p<0.05, compared with the GES-1 groups. 

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]


Kinase Assay:


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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:


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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:


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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.
  • 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)
Water Insoluble
Ethanol '2 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

* 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

C17 H12 N2 O

CAS No. 4382-63-2
Storage powder
in solvent
Synonyms PFK-015
Smiles C1=CC=C2C(=C1)C=CC(=N2)C=CC(=O)C3=CC=NC=C3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID