Key Spec Table
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|5.31005.0001||Glass bottle||25 mg||
|Overview||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.
|Synonyms||(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|
|References||Clem, B. F., et al. 2013. Mol. Cancer Ther. 12, 1461.|
|Form||Light beige solid|
|Primary Target IC<sub>50</sub>||207 nM for hrPFKFP3|
|Purity||≥97% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
PFKFB3 Inhibitor II, PFK15 - Calbiochem SDS
|Clem, B. F., et al. 2013. Mol. Cancer Ther. 12, 1461.|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.