PFK15

Catalog No.S7289

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

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PFK15 Chemical Structure

PFK15 Chemical Structure
Molecular Weight: 260.29

Validation & Quality Control

Quality Control & MSDS

Product Information

Product Description

Biological Activity

Description PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) with IC50 of 207 nM.
Targets PFKFB3 [1]
IC50 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]
Features

Protocol(Only for 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's instructions and fluorescent and FRET signals are measured on a Tecan Safire2 plate reader. Graphs are generated using SigmaPlot software and IC50 values are calculated using a 3-parameter Hill Equation.

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.
Formulation DMSO
Dosages 25 mg/kg every 3 days
Administration i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Clem BF, et al. Mol Cancer Ther. 2013, 12(8), 1461-1470.

Chemical Information

Download PFK15 SDF
Molecular Weight (MW) 260.29
Formula

C17 H12 N2 O

CAS No. 4382-63-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms PFK-015
Solubility (25°C) * In vitro DMSO 19 mg/mL warmed (72.99 mM)
Ethanol 2 mg/mL warmed (7.68 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <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.
Chemical Name 2-​Propen-​1-​one, 1-​(4-​pyridinyl)​-​3-​(2-​quinolinyl)​-

Tech Support

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
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