ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors PFK-158

PFK-158

Product NamePFK-158
CAS1462249-75-7
MFC18H11F3N2O
MW328.29
EINECS
MOL File1462249-75-7.mol

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

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

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.

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