- PFK-158
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- $30.00
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2026-07-14
- CAS:1462249-75-7
- Purity: 98.88%
- Supply Ability: 10g
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| | 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 | | InChI | 1S/C18H11F3N2O/c19-18(20,21)14-3-1-12-2-4-15(23-16(12)11-14)5-6-17(24)13-7-9-22-10-8-13/h1-11H/b6-5+ | | InChIKey | IAJOMYABKVAZCN-AATRIKPKSA-N | | SMILES | O=C(/C=C/C1=NC2=C(C=CC(C(F)(F)F)=C2)C=C1)C3=CC=NC=C3 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | 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.
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| | 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-158 Preparation Products And Raw materials |
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