|
|
| | PFK-158 Basic information |
| Product Name: | PFK-158 | | Synonyms: | PFK-158;PFK-158, ACT-PFK-158;(2E)-1-(4-Pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-2-propen-1-one;PFK-158;PFK 158;PFK-158 free base;2-Propen-1-one, 1-(4-pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-, (2E)-;(E)-1-(Pyridin-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)prop-2-en-1-one;p-cPLA2,inhibit,anti-proliferative,Autophagy,PFK 158,LC3BII,glycolysis,Inhibitor,PFK158,anti-tumor,PFK-158,Apoptosis,lactate,PFKFB3 | | CAS: | 1462249-75-7 | | MF: | C18H11F3N2O | | MW: | 328.29 | | EINECS: | | | Product Categories: | | | Mol File: | 1462249-75-7.mol |  |
| | PFK-158 Chemical Properties |
| Boiling point | 466.3±45.0 °C(Predicted) | | density | 1.346±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:14.0(Max Conc. mg/mL);42.6(Max Conc. mM) | | form | A crystalline solid | | pka | 2.46±0.10(Predicted) | | color | White to light yellow |
| | PFK-158 Usage And Synthesis |
| Description | PFK158 is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3; IC50 = 137 nM for human recombinant PFKFB3). It inhibits PFKFB3 and glycolysis in Jurkat cells (IC50s = 1.6 and 0.847 μM, respectively). PFK158 inhibits the growth of leukemia cells in vitro (IC50 = 0.33 μM for Jurkat cells) and reduces tumor volume in CT-26 murine colon carcinoma syngeneic model and a BxPC-3 pancreatic cancer mouse xenograft model. PFK158 also enhances activity of the anti-CTLA-4 antibody in the B16/F10 mouse model of melanoma. |
| | PFK-158 Preparation Products And Raw materials |
|