PFK-158
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
- 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.
Uses
PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria[1][2][3].
in vivo
PFK-158 (15 mg/kg; intraperitoneal injection; once a week; for 4 weeks; female athymic nude mice) plus CBPt (51 mg/kg) treatment leads to significantly enhanced antitumor activity in a gynecologic cancer mouse model[1].
| Animal Model: | Female athymic nude mice (nu/nu) (5-6 weeks old) injected with HeyA8MDR cells[1] |
| Dosage: | 15 mg/kg |
| Administration: | Intraperitoneal injection; once a week; for 4 weeks |
| Result: | A marked reduction of tumor growth was observed in the combination treatment. |
References
[1] Mondal S, et al. Therapeutic targeting of PFKFB3 with a novel glycolytic inhibitor PFK158 promotes lipophagy and chemosensitivity in gynecologic cancers. Int J Cancer. 2019 Jan 1;144(1):178-189. DOI:10.1002/ijc.31868
[2] Zhang Y, et al. Synergistic Effect of Colistin Combined with PFK-158 against Colistin-Resistant Enterobacteriaceae. Antimicrob Agents Chemother. 2019 Jun 24;63(7). pii: e00271-19. DOI:10.1128/AAC.00271-19
[3] Pooran Chand, et al. Pfkfb3 inhibitor and methods of use as an anti-cancer therapeutic. WO2013148228A1.
PFK-158Supplier
- Tel
- sales@boylechem.com
- Tel
- 025-58849295 18951903616;
- info@adooq.cn
- Tel
- 13621943973
- sales@shjiyipharmatech.com
- Tel
- 400-026-9899
- Tel
- 021-52996696，15000506266 15000506266