5.31005

PFKFB3 Inhibitor II, PFK15

• Synonym(s): PFKFB3 Inhibitor II, PFK15, ( E)-1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one, 1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one, 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 Inhibitor, PFK15, (E)-1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one, 1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one, 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 Inhibitor, PFK15
• Empirical Formula (Hill Notation): C₁₇H₁₂N₂O
• CAS Number: 4382-63-2
• Molecular Weight: 260.29
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥97% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light beige
• solubility: DMSO: 10 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell-permeable, bioavailable and more potent quinolinyl analog of PFKFB3 Inhibitor, 3PO (Cat. No. 525330) that inhibits the activity of 6-Phosphofructo-2-kinase (PFKFB3) by reversibly docking to its substrate binding domain (IC₅₀ = 207 nM compared to 22.9 µM for 3PO). Shown to effectively reduce fructose 2,6-bisphosphate, glucose uptake, and intracellular ATP levels. Does neither affect the activity of 96 other kinases in any significant manner (at ~10 µM) nor PFK-1, hexokinase, phosphoglucoisomerase, or PFKFB4 even at 100 µM. Induces apoptosis and reduces proliferation in transformed cells (mean GI₅₀ of ~3 µM in the NCI-60 cancer cell panel). Displays adequate pharmacokinetic properties to suppress glucose uptake and the growth of Lewis lung carcinoma is syngenic mice and block the growth of human tumor xenografts in athymic mice (~25 mg/kg, i.p. administered every 3rd day).

A cell-permeable, bioavailable and more potent quinolinyl analog of PFKFB3 Inhibitor, 3PO (Cat. No. 525330) that inhibits the activity of 6-Phosphofructo-2-kinase (PFKFB3) by reversibly docking to its substrate binding domain (IC₅₀ = 207 nM compared to 22.9 µM for 3PO). Shown to effectively reduce fructose 2,6-bisphosphate, glucose uptake, and intracellular ATP levels. Does neither affect the activity of 96 other kinases in any significant manner (at ~10 µM) nor PFK-1, hexokinase, phosphoglucoisomerase, or PFKFB4 even at 100 µM. Induces apoptosis and reduces proliferation in transformed cells (mean GI₅₀ of ~3 µM in the NCI-60 cancer cell panel). Displays adequate pharmacokinetic properties to suppress glucose uptake and the growth of Lewis lung carcinoma is syngenic mice and block the growth of human tumor xenografts in athymic mice (~25 mg/kg, i.p. administered every 3rd day).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PFKFB3

Reversible: yes

Target IC₅₀: 207 nM for hrPFKFP3

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Use only fresh DMSO for reconstitution.

Other Notes

Clem, B. F., et al. 2013. Mol. Cancer Ther.12, 1461.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable