product name PFK-015
Description: PFK-015 (also known as PFK15) is a novel, potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM. 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.
References: Mol Cancer Ther. 2013 Aug;12(8):1461-70.
260.29
Formula
C17H12N2O
CAS No.
4382-63-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 19 mg/mL (73 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (7.67mM)
Solubility (In vivo)
5% DMSO+45% PEG 300+1% Tween 80+ddH2O: 5mg/mL
Synonyms
PFK-015
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase 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 Assay: 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. |
|---|---|
| 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. |
| Animal model | C57Bl/6 mice bearing LLC xenografts, Balb/C athymic mice bearing CT26, U-87 MG, or BxPC-3 xenografts. |
| Formulation & Dosage | Dissolved in DMSO; 25 mg/kg every 3 days; i.p. injection |
| References | Mol Cancer Ther. 2013 Aug;12(8):1461-70. |
