PFK15

Name: PFK15
Brand: Selleck Chemicals
SKU: S7289
Rating: 5 (9 reviews)

For research use only.

Catalog No.S7289 Synonyms: PFK-015

9 publications

Molecular Weight(MW): 260.29

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

Selleck's PFK15 has been cited by 9 publications

ACS Appl Mater Interfaces, 2020, 6

PubMed: 32330381 ( click the link to review the publication )

J Cell Mol Med, 2020, 24(3):2294-2307

PubMed: 31880389 ( click the link to review the publication )

IUBMB Life, 2020, 10.1002/iub.2232

PubMed: 31958214 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 515(2):332-338

PubMed: 31153642 ( click the link to review the publication )

Nat Commun, 2018, 9(1):508

PubMed: 29410405 ( click the link to review the publication )

Oncogene, 2018, 37(21):2837-2849

PubMed: 29511345 ( click the link to review the publication )

Br J Pharmacol, 2017, 174(9):893-908

PubMed: 28239846 ( click the link to review the publication )

J Exp Clin Cancer Res, 2017, 10.1186/s13046-016-0481-1

PubMed: 28061878 ( click the link to review the publication )

PLoS One, 2016, 11(9):e0163768

PubMed: 27669567 ( click the link to review the publication )

3 Customer Reviews

b EdU incorporation assays indicated PFK15 inhibited the cell proliferation of Cal27 cells. c The quantitative data of the EdU incorporation assays.

J Exp Clin Cancer Res, 2017, 36(1):7. PFK15 purchased from Selleck.

RA FLSs were pretreated with DMSO (as the control) or various concentrations of a specific PFKFB3 inhibitor, PFK15, for 4 h (A). The expression of IL-6, IL-8, CCL-2 and CXCL-10 was measured by real-time qPCR. The data are representative of independent experiments (means ± SEM) from10 RA patients. *P < 0.05, significantly different from control or SiC; #P < 0.05, significantly different from treatment with TNF-α alone

Br J Pharmacol, 2017, 174(9):893-908. PFK15 purchased from Selleck.
(a, b) Cells were treated with the indicated concentrations of PFK15 for 12 h in the upper chambers and the lower chambers were filled with 10% FBS medium. Then, the invaded cells were stained with crystal violet and observed under a microscope with 200× magnification. Data were obtained from six randomly chosen fields and were normalized to the control group. (c) Proteins related with cell migration and invasion were detected. Phospho-FAK levels were downregulated in 7 and 9 μM while phospho-Cadherin E levels upregulated in both cell lines. Columns, mean; bars, SD. *P<0.05, compared with controls.

PLoS One, 2016, 11(9):e0163768. PFK15 purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description

PFK15 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]

Assay

Methods	Test Index	PMID
Western blot	Cyclin E1 / CDK2 / Cyclin D1 / CDK4 / CDK6 / E2F1 / Rb / p-Rb ; PubMed: 27669567 PLoS One Cells were treated with various concentration of PFK15 for 24 h. The cell cycle associated proteins were checked by western bolt assay. PFK15 treatment significantly decreased expressions of cyclin D1, cyclin E1, phosphorylated Rb and the nuclear transfactor E2F-1 levels while increased non-phosphorylated Rb protein levels in both MKN45 and AGS cell lines.	27669567
Growth inhibition assay	Cell viability; PubMed: 27669567 PLoS One Cells grown in exponential phase were exposed to the indicated concentrations of PFK15 and, after 24 h, the effects on viability were determined by trypan blue exclusion. *p<0.05, compared with the GES-1 groups.	27669567

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

Kinase Assay: ^[1]	- Collapse 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: ^[1]	- Collapse 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. (Only for Reference)
Animal Research: ^[1]	- Collapse 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. (Only for Reference)

References

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

Solubility (25°C)

In vitro	DMSO	19 mg/mL warmed (72.99 mM)
	Ethanol	2 mg/mL warmed (7.68 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+45% PEG 300+1% Tween 80+ddH2O For best results, use promptly after mixing.	5mg/mL

* 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 Information Download PFK15 SDF

Molecular Weight	260.29
Formula	C₁₇ H₁₂ N₂ O
CAS No.	4382-63-2
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	PFK-015
Smiles	O=C(\C=C\C1=CC=C2C=CC=CC2=N1)C3=CC=NC=C3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

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The Serial Dilution Calculator Equation

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Molecular Weight Calculator

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PFK15