PFKFB3 抑制剂，3PO-Calbiochem

C₁₃H₁₀N₂O

210.23

MFCD00224002

A cell-permeable dipyridinyl-propenone compound that selectively blocks PFK-2 (6-phosphofructo-2-kinase) activity of PFKFB3 isozyme over PFK-1(6-phosphofructo-1-kinase) in a mixed-mode manner. Rapidly decreases fructose-2,6-bisphosphate (F-2,6-P₂) and 2-deoxyglucose uptake, and lactate secretion; efficiently arrests proliferation of transformed cells (IC₅₀ ~ 1.4 µM in NHBE-ht/LT/ras) and suppresses tumor growth in several xenograft mouse models (70 mg/kg, i.p.). The cytostatic and cytotoxic effects of 3PO is shown to be highly sensitive to the intracellular levels of F-6-P (fructose-6-phosphate) and F-2,6-P₂.

Toxicity: Standard Handling (A)

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

Clem, B., et al. 2008. Mol. Cancer Ther.7, 110.

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

100

≥99% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

pale yellow

DMSO: 50 mg/mL

ambient

2-8℃

25 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3