Home >> Research Area >> PFK-015

PFK-015

PFKFB3 inhibitor, potent and selective CAS# 4382-63-2

PFK-015

Catalog No. BCC5280----Order now to get a substantial discount!

Product Name & Size Price Stock
PFK-015: 5mg $897 In Stock
PFK-015: 10mg Please Inquire In Stock
PFK-015: 20mg Please Inquire Please Inquire
PFK-015: 50mg Please Inquire Please Inquire
PFK-015: 100mg Please Inquire Please Inquire
PFK-015: 200mg Please Inquire Please Inquire
PFK-015: 500mg Please Inquire Please Inquire
PFK-015: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of PFK-015

Number of papers citing our products

Chemical structure

PFK-015

3D structure

Chemical Properties of PFK-015

Cas No. 4382-63-2 SDF Download SDF
PubChem ID 25142799 Appearance Powder
Formula C17H12N2O M.Wt 260.29
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 25.2 mg/mL (96.82 mM; Need ultrasonic and warming)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name (E)-1-pyridin-4-yl-3-quinolin-2-ylprop-2-en-1-one
SMILES C1=CC=C2C(=C1)C=CC(=N2)C=CC(=O)C3=CC=NC=C3
Standard InChIKey UJJUKZPBUMCSJZ-BQYQJAHWSA-N
Standard InChI InChI=1S/C17H12N2O/c20-17(14-9-11-18-12-10-14)8-7-15-6-5-13-3-1-2-4-16(13)19-15/h1-12H/b8-7+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PFK-015

DescriptionOriginally reported to be a selective PFKFB3 inhibitor (IC50 = 207 nM); a more recent report failed to demonstrate activity in a PFKFB3 kinase assay. Selective for PFKFB3 over a panel of 96 kinases. Reduces glucose uptake and induces apoptosis in H522 lung adenocarcinoma and Jurkat T cell leukemia cells. Suppresses glucose uptake and tumor growth, and inhibits metastasis of Lewis lung carcinoma cell xenografts in mice.

PFK-015 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

PFK-015 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of PFK-015

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.8419 mL 19.2093 mL 38.4187 mL 76.8374 mL 96.0467 mL
5 mM 0.7684 mL 3.8419 mL 7.6837 mL 15.3675 mL 19.2093 mL
10 mM 0.3842 mL 1.9209 mL 3.8419 mL 7.6837 mL 9.6047 mL
50 mM 0.0768 mL 0.3842 mL 0.7684 mL 1.5367 mL 1.9209 mL
100 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.7684 mL 0.9605 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on PFK-015

PFK-015 is a potent and selective inhibitor of PFKFB3 with IC50 value of 207 nM [1].

6-phosphofructo-2-kinase (PFKFB3) is an enzyme that is encoded by the PFKFB3 gene in humans. PFKFB3 is a direct transcriptional target of HIF-α and is activated by oncogenic AKT and Ras and stabilized by the loss of the tumor suppressor PTEN via suppressive effects on APC/Cdh1-mediated ubiquitination [1].

PFK-015 is a potent and selective PFKFB3 inhibitor. In H522 lung adenocarcinoma and Jurkat cell lines, PFK15 exhibited cytotoxic effects with IC50 values of 2.42 and 0.72 μM in Jurkat and H522, respectively. Also, PFK15 reduced glucose uptake, intracellular ATP and F26BP, the substrate of PFKFB3. In Jurkat T cell leukemia cells, PFK15 (3 μM) increased the number of cells undergoing early apoptosis. PFK15 (3 and 20 μM) increased the number of cells undergoing late apoptosis in a dose dependent way [1].

In Lewis lung carcinoma (LLC)-bearing mice, PFK15 inhibited LLC cells metastasized from the subcutaneous to the lungs. PFK15 decreased tumor-associated F26BP and significantly increased the number of cells that were positive for cleaved caspase 3. Also, PFK15 reduced fluoro-D-glucose (18F-FDG) uptake by 50%. PFK15 inhibited the growth of colon and pancreatic adenocarcinomas [1].

Reference:
[1].  Clem BF, O'Neal J, Tapolsky G, et al. Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer. Mol Cancer Ther, 2013, 12(8): 1461-1470.

Featured Products
New Products
 

References on PFK-015

Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer.[Pubmed:23674815]

Mol Cancer Ther. 2013 Aug;12(8):1461-70.

In human cancers, loss of PTEN, stabilization of hypoxia inducible factor-1alpha, and activation of Ras and AKT converge to increase the activity of a key regulator of glycolysis, 6-phosphofructo-2-kinase (PFKFB3). This enzyme synthesizes fructose 2,6-bisphosphate (F26BP), which is an activator of 6-phosphofructo-1-kinase, a key step of glycolysis. Previously, a weak competitive inhibitor of PFKFB3, 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one (3PO), was found to reduce the glucose metabolism and proliferation of cancer cells. We have synthesized 73 derivatives of 3PO and screened each compound for activity against recombinant PFKFB3. One small molecule, 1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one (PFK15), was selected for further preclinical evaluation of its pharmacokinetic, antimetabolic, and antineoplastic properties in vitro and in vivo. We found that PFK15 causes a rapid induction of apoptosis in transformed cells, has adequate pharmacokinetic properties, suppresses the glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in three human xenograft models of cancer in athymic mice that are comparable to U.S. Food and Drug Administration-approved chemotherapeutic agents. As a result of this study, a synthetic derivative and formulation of PFK15 has undergone investigational new drug (IND)-enabling toxicology and safety studies. A phase I clinical trial of its efficacy in advanced cancer patients will initiate in 2013 and we anticipate that this new class of antimetabolic agents will yield acceptable therapeutic indices and prove to be synergistic with agents that disrupt neoplastic signaling.

Description

PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.

Keywords:

PFK-015,4382-63-2,Natural Products, buy PFK-015 , PFK-015 supplier , purchase PFK-015 , PFK-015 cost , PFK-015 manufacturer , order PFK-015 , high purity PFK-015

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: