PFK15

Catalog No.S7289 Batch:S728901

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Technical Data

Formula

C17 H12 N2 O
Molecular Weight 260.29 CAS No. 4382-63-2
Solubility (25°C)* In vitro DMSO 19 mg/mL (72.99 mM)
Ethanol 2 mg/mL (7.68 mM)
Water Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

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

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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.
Animal Study:

[1]
  • 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.

Customer Product Validation

, , J Exp Clin Cancer Res, 2017, 36(1):7

Data from [Data independently produced by , , Br J Pharmacol, 2017, 174(9):893-908]

Data from [Data independently produced by , , PLoS One, 2016, 11(9):e0163768]

Selleck's PFK15 has been cited by 30 publications

Identification of PFKFB3 as a key factor in the development of colorectal cancer and immunotherapy resistance [ Clin Exp Med, 2024, 24(1):219] PubMed: 39261380
Multi-omics and immunogenomics analysis revealed PFKFB3 as a targetable hallmark and mediates sunitinib resistance in papillary renal cell carcinoma: in silico study with laboratory verification [ Eur J Med Res, 2024, 29(1):236] PubMed: 38622715
Human blood vessel organoids reveal a critical role for CTGF in maintaining microvascular integrity [ Nat Commun, 2023, 14(1):5552] PubMed: 37689702
Human blood vessel organoids reveal a critical role for CTGF in maintaining microvascular integrity [ Nat Commun, 2023, 14(1):5552] PubMed: 37689702
Arginine methylation of PPP1CA by CARM1 regulates glucose metabolism and affects osteogenic differentiation and osteoclastic differentiation [ Clin Transl Med, 2023, 13(9):e1369] PubMed: 37649137
Arginine methylation of PPP1CA by CARM1 regulates glucose metabolism and affects osteogenic differentiation and osteoclastic differentiation [ Clin Transl Med, 2023, 13(9):e1369] PubMed: 37649137
PFKFB3-mediated Pro-glycolytic Shift in Hepatocellular Carcinoma Proliferation [ Cell Mol Gastroenterol Hepatol, 2023, 15(1):61-75] PubMed: 36162723
Long noncoding RNA LINC00930 promotes PFKFB3-mediated tumor glycolysis and cell proliferation in nasopharyngeal carcinoma [ J Exp Clin Cancer Res, 2022, 41(1):77] PubMed: 35209949
CYLD deficiency enhances metabolic reprogramming and tumor progression in nasopharyngeal carcinoma via PFKFB3 [ Cancer Lett, 2022, S0304-3835(22)00055-6] PubMed: 35131382
Metabolic reprogramming by dual-targeting biomimetic nanoparticles for enhanced tumor chemo-immunotherapy [ Acta Biomater, 2022, 148:181-193] PubMed: 35649505

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.