PFK-015
PFK-015 Basic information
- Product Name:
- PFK-015
- Synonyms:
-
- PFK015;PFK15;PFK 15;PFK-15
- CS-1317
- 2-Propen-1-one, 1-(4-pyridinyl)-3-(2-quinolinyl)-
- 1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one PFK15
- 1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one
- PFK15 (PFK-015)
- PFK-015
- 1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
- CAS:
- 4382-63-2
- MF:
- C17H12N2O
- MW:
- 260.29
- Product Categories:
-
- Inhibitors
- Mol File:
- 4382-63-2.mol
PFK-015 Chemical Properties
- Boiling point:
- 464.4±45.0 °C(Predicted)
- Density
- 1.237±0.06 g/cm3(Predicted)
- storage temp.
- Sealed in dry,2-8°C
- solubility
- DMSO: soluble10mg/mL, clear
- form
- powder
- pka
- 3.11±0.61(Predicted)
- color
- white to beige
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Safety Information
- Hazard Codes
- Xi
- Risk Statements
- 36/37/38
- Safety Statements
- 26-36/37/39
- WGK Germany
- 3
PFK-015 Usage And Synthesis
Description
PFK15 (4382-63-2) is an inhibitor of the metabolic enzyme 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3).? PFKFB3 is constitutively expressed by neoplastic cells and is required for the high glycolytic rate (Warburg Effect) of these cells. PFK15 inhibits PFKFB3 (IC50?= 207 nM) without inhibiting 96 other kinases.1?PFK15 was able to potently inhibit glucose and F26BP uptake. It induced apoptosis and reduced tumor growth?in vitro?and?in vivo.?PFK15 has been shown to inhibit tumor growth in various cancer models.2,3
Uses
PFK 15 is a novel inhibitor of glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). It suppresses the glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and induces apoptosis in abnormal cells.
in vivo
PFK-015 impeds ESCC tumor growth in immunodeficient in vivo models[1].
? ?
PFK-015 (0-12.5 μM, 48 h) induces tumor PD-L1 expression[1].
? ?
PFK-015 (0-12.5 μM, 48 h) can cause a downregulation of immune activity against tumor cells mediated by CD8 + T cells[1].
? ?
PFK-015 enhances the efficacy of ESCC by enhancing CD8 + T-cell activity combining PD-1 mAb in immunocompetent mouse models such as C57BL/6 and hu-PBMC-NOG[1].
?
PFK-015 (iv, 5 mg/kg) has a satisfactory half-life, exposure, tissue distribution and reasonable clearance[2].
storage
Store at -20°C
References
[1] BRIAN F CLEM. Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer.[J]. Molecular Cancer Therapeutics, 2013, 12 8: 1461-1470. DOI:10.1158/1535-7163.mct-13-0097
[2] WEI ZHU. PFK15, a Small Molecule Inhibitor of PFKFB3, Induces Cell Cycle Arrest, Apoptosis and Inhibits Invasion in Gastric Cancer[J]. PLoS ONE, 2016, 11 1. DOI:10.1371/journal.pone.0163768
[3] HUI-MIN LI. Blockage of glycolysis by targeting PFKFB3 suppresses tumor growth and metastasis in head and neck squamous cell carcinoma.[J]. Progress in brain research, 2017, 5 1: 7. DOI:10.1186/s13046-016-0481-1
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