ChemicalBook > CAS DataBase List > PFK-158

PFK-158

Product Name
PFK-158
CAS No.
1462249-75-7
Chemical Name
PFK-158
Synonyms
PFK-158;PFK-158;PFK 158;PFK-158 free base;PFK-158, ACT-PFK-158;PFK-158, 10 mM in DMSO;(E)-1-(4-Pyridyl)-3-[7-(trifluoromethyl)-2-quinolyl]-2-propen-1-one;(2E)-1-(4-Pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-2-propen-1-one;(E)-1-(Pyridin-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)prop-2-en-1-one;2-Propen-1-one, 1-(4-pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-, (2E)-;p-cPLA2,inhibit,anti-proliferative,Autophagy,PFK 158,LC3BII,glycolysis,Inhibitor,PFK158,anti-tumor,PFK-158,Apoptosis,lactate,PFKFB3
CBNumber
CB43034954
Molecular Formula
C18H11F3N2O
Formula Weight
328.29
MOL File
1462249-75-7.mol
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PFK-158 Property

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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3145
Product name
PFK-158
Purity
≥98% (HPLC)
Packaging
5MG
Price
$86.92
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3145
Product name
PFK-158
Purity
≥98% (HPLC)
Packaging
25MG
Price
$295
Updated
2025/07/31
Cayman Chemical
Product number
22987
Product name
PFK158
Purity
≥95%
Packaging
5mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
22987
Product name
PFK158
Purity
≥95%
Packaging
10mg
Price
$107
Updated
2024/03/01
Cayman Chemical
Product number
22987
Product name
PFK158
Purity
≥95%
Packaging
25mg
Price
$220
Updated
2024/03/01
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PFK-158 Chemical Properties,Usage,Production

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-158 Preparation Products And Raw materials

Raw materials

Preparation Products

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PFK-158 Suppliers

China 71 United States 8 Global 79
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
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55
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
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60
Shanghai JiYi Biotechnology Co. Ltd.
Tel
13621943973
Fax
-
Email
sales@shjiyipharmatech.com
Country
China
ProdList
1166
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55
Hunan Cangood Medical Technology Ltd.
Tel
400-026-9899
Fax
+86-731-86905278
Country
China
ProdList
71
Advantage
50
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
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55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
984
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55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
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58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
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60
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2989
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58
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9125
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58

1462249-75-7, PFK-158Related Search:

PFK-015 Silver

  • 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
  • (E)-1-(4-Pyridyl)-3-[7-(trifluoromethyl)-2-quinolyl]-2-propen-1-one
  • PFK-158, 10 mM in DMSO
  • 1462249-75-7
  • 1462249-75-1
  • C18H11F3N2O