PFK-015

Product NamePFK-015
CAS4382-63-2
MFC17H12N2O
MW260.29
EINECS
MOL File4382-63-2.mol

Chemical Properties

Boiling point	464.4±45.0 °C(Predicted)
Density	1.237±0.06 g/cm3(Predicted)
storage temp.	Sealed in dry,2-8°C
solubility	DMSO: soluble10mg/mL, clear
pka	3.11±0.61(Predicted)
form	powder
color	white to beige
Stability	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
InChI	1S/C17H12N2O/c20-17(14-9-11-18-12-10-14)8-7-15-6-5-13-3-1-2-4-16(13)19-15/h1-12H/b8-7+
InChIKey	UJJUKZPBUMCSJZ-BQYQJAHWSA-N
SMILES	n1ccc(cc1)C(=O)\C=C\c2nc3c(cc2)cccc3

Safety Information

Hazard Codes	Xi
Risk Statements	36/37/38
Safety Statements	26-36/37/39
WGK Germany	3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Description

PFK15 (4382-63-2) is an inhibitor of the metabolic enzyme 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3). PFKFB3 is constitutively expressed by neoplastic cells and is required for the high glycolytic rate (Warburg Effect) of these cells. PFK15 inhibits PFKFB3 (IC50= 207 nM) without inhibiting 96 other kinases.1PFK15 was able to potently inhibit glucose and F26BP uptake. It induced apoptosis and reduced tumor growthin vitroandin vivo.PFK15 has been shown to inhibit tumor growth in various cancer models.2,3

Uses

PFK 15 is a novel inhibitor of glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). It suppresses the glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and induces apoptosis in abnormal cells.

in vivo

PFK-015 impeds ESCC tumor growth in immunodeficient in vivo models^[1].
PFK-015 (0-12.5 μM, 48 h) induces tumor PD-L1 expression^[1].
PFK-015 (0-12.5 μM, 48 h) can cause a downregulation of immune activity against tumor cells mediated by CD8 ⁺ T cells^[1].
PFK-015 enhances the efficacy of ESCC by enhancing CD8 ⁺ T-cell activity combining PD-1 mAb in immunocompetent mouse models such as C57BL/6 and hu-PBMC-NOG^[1].
PFK-015 (iv, 5 mg/kg) has a satisfactory half-life, exposure, tissue distribution and reasonable clearance^[2].

storage

Store at -20°C

References

[1] BRIAN F CLEM. Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer.[J]. Molecular Cancer Therapeutics, 2013, 12 8: 1461-1470. DOI:10.1158/1535-7163.mct-13-0097
[2] WEI ZHU. PFK15, a Small Molecule Inhibitor of PFKFB3, Induces Cell Cycle Arrest, Apoptosis and Inhibits Invasion in Gastric Cancer[J]. PLoS ONE, 2016, 11 1. DOI:10.1371/journal.pone.0163768
[3] HUI-MIN LI. Blockage of glycolysis by targeting PFKFB3 suppresses tumor growth and metastasis in head and neck squamous cell carcinoma.[J]. Progress in brain research, 2017, 5 1: 7. DOI:10.1186/s13046-016-0481-1

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