PFK-015

Synonym(s):1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one

CAS NO.：4382-63-2
Empirical Formula: C17H12N2O
Molecular Weight: 260.29
MDL number: MFCD28099813
SAFETY DATA SHEET (SDS)
Update Date: 2024-11-19 23:02:33

What is PFK-015?

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.1?PFK15 was able to potently inhibit glucose and F26BP uptake. It induced apoptosis and reduced tumor growth?in vitro?and?in vivo.?PFK15 has been shown to inhibit tumor growth in various cancer models.2,3

The Uses of PFK-015

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.

storage

Store at -20°C

References

1) Clem?et al.?(2013),?Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer; Mol. Cancer Ther.?12?1461 2) Zhu?et al. (2016),?PFK15,a Small Molecule Inhibitor of PFKFB3, Induces Cell Cycle Arrest, Apoptosis and Inhibits Invasion in Gastric Cancer; PLoS One?11?e0163768 3) Li?et al. (2017),?Blockage of glycolysis by targeting PFKFB3 suppresses tumor growth and metastasis in head and neck squamous cell carcinoma; J. Exp. Clin. Cancer Res.?36?7

Properties of PFK-015

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
form	powder
pka	3.11±0.61(Predicted)
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.

Safety information for PFK-015

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.