PFK158

Catalog No.S8807 Batch:S880702

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Technical Data

Formula

C18H11F3N2O
Molecular Weight 328.29 CAS No. 1462249-75-7
Solubility (25°C)* In vitro DMSO 66 mg/mL (201.04 mM)
Ethanol 4 mg/mL (12.18 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
3.3mg/ml Taking the 1 mL working solution as an example, add 50 μL of 66 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.3mg/ml Taking the 1 mL working solution as an example, add 50 μL of 66 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. 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 PFK158 is a potent and selective inhibitor of PFKFB3. It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors.
Targets
PFKFB3 [1]
In vitro

PFK158 results in reduced glucose uptake, ATP production, lactate release as well as induction of apoptosis in gynecologic cancer cells. PFK158 treatment sensitizes chemoresistant cells and induces cell death[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Female athymic nude mice (nu/nu) (5-6 weeks old)

  • Dosages

    25 mg/kg

  • Administration

    i.p.

Selleck's PFK158 has been cited by 7 publications

Microglial hexokinase 2 deficiency increases ATP generation through lipid metabolism leading to β-amyloid clearance [ Nat Metab, 2022, 4(10):1287-1305] PubMed: 36203054
Glycolysis Dependency as a Hallmark of SF3B1-Mutated Cells [ Cancers (Basel), 2022, 14(9)2113] PubMed: 35565242
In Vivo Targeting Replication Protein A for Cancer Therapy [ Front Oncol, 2022, 12:826655] PubMed: 35251993
Glycolysis Inhibition Induces Functional and Metabolic Exhaustion of CD4+ T Cells in Type 1 Diabetes [ Front Immunol, 2021, 12:669456] PubMed: 34163475
Glycolysis Inhibition Induces Functional and Metabolic Exhaustion of CD4+ T Cells in Type 1 Diabetes [ Front Immunol, 2021, 12:669456] PubMed: 34163475
Targeting MYC-enhanced glycolysis for the treatment of small cell lung cancer [ Cancer Metab, 2021, 9(1):33] PubMed: 34556188
Deamidation Shunts RelA From Mediating Inflammation to Aerobic Glycolysis [ Cell Metab, 2020, 5;31(5):937-955e7] PubMed: 32325032

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.