PFK15

Catalog No.S7289 Batch:S728904

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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 5 mg/mL (19.2 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% corn oil
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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 26 publications

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
PFKFB3 mediates tubular cell death in cisplatin nephrotoxicity by activating CDK4 [ Transl Res, 2022, S1931-5244(22)00220-1] PubMed: 36243313
Increased stromal PFKFB3-mediated glycolysis in inflammatory bowel disease contributes to intestinal inflammation [ Front Immunol, 2022, 13:966067] PubMed: 36405760
Glucose metabolism inhibitor PFK-015 combined with immune checkpoint inhibitor is an effective treatment regimen in cancer [ Oncoimmunology, 2022, 11(1):2079182] PubMed: 35707221

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.