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PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $52 | In Stock | |
10 mg | $81 | In Stock | |
25 mg | $162 | In Stock | |
50 mg | $297 | In Stock | |
100 mg | $441 | In Stock | |
200 mg | $612 | In Stock | |
500 mg | $976 | In Stock | |
1 mL x 10 mM (in DMSO) | $52 | In Stock |
Description | PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM). |
Targets&IC50 | PFKFB3:110 nM, PFKFB3:20 nM |
In vitro | PFK-015 (25 mg/kg, i.p.) inhibits the growth, metastatic spread, and glucose metabolism of LLC tumors in syngeneic mice. In three distinct athymic mouse models of xenografted human cancers, the anticancer efficacy of PFK-015 is comparable to that of established chemotherapy drugs. PFK-015 exhibits favorable pharmacokinetic properties in vivo. |
In vivo | PFK-015 effectively reduces levels of F26BP, glucose uptake, and intracellular adenosine triphosphate (ATP) in Jurkat T-cell leukemia cells and H522 lung adenocarcinoma cells. Additionally, PFK-015 exhibits significant inhibitory effects on the growth of a variety of cancer cells. |
Kinase Assay | 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 | 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) |
Alias | PFK15, PFK 015 |
Molecular Weight | 260.29 |
Formula | C17H12N2O |
Cas No. | 4382-63-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 3 mg/mL (11.53 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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