| Identification | Back Directory | [Name]
PFK-158 | [CAS]
1462249-75-7 | [Synonyms]
PFK-158
PFK-158;PFK 158
PFK-158 free base
PFK-158, ACT-PFK-158
(2E)-1-(4-Pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-2-propen-1-one
2-Propen-1-one, 1-(4-pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-, (2E)- | [Molecular Formula]
C18H11F3N2O | [MOL File]
1462249-75-7.mol | [Molecular Weight]
328.29 |
| Chemical Properties | Back Directory | [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) |
| Hazard Information | Back Directory | [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. |
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