531005 Sigma-AldrichPFKFB3 Inhibitor II, PFK15 - CAS 4382-63-2 - Calbiochem
A cell-permeable inhibitor of PFKFB3 that reversibly docks to its substrate binding domain (IC₅₀ = 207 nM)
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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
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Overview
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Key Spec Table
| CAS # | Empirical Formula |
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| 4382-63-2 | C₁₇H₁₂N₂O |
Pricing & Availability
| Catalogue Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
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| 5.31005.0001 |
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Botol kaca | 25 mg |
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| Description | |
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| 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. |
| Catalogue Number | 531005 |
| Brand Family | Calbiochem® |
| 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 | |
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| References | Clem, B. F., et al. 2013. Mol. Cancer Ther. 12, 1461. |
| Product Information | |
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| CAS number | 4382-63-2 |
| Form | Light beige solid |
| Hill Formula | C₁₇H₁₂N₂O |
| Chemical formula | C₁₇H₁₂N₂O |
| Reversible | Y |
| Quality Level | MQ100 |
| Applications |
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| Biological Information | |
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| Primary Target | PFKFB3 |
| Primary Target IC<sub>50</sub> | 207 nM for hrPFKFP3 |
| Purity | ≥97% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Materials Information |
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| Toxicological Information |
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| Safety Information according to GHS |
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| Safety Information |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Catalogue Number | GTIN |
| 5.31005.0001 | 04055977242492 |
Documentation
PFKFB3 Inhibitor II, PFK15 - CAS 4382-63-2 - Calbiochem MSDS
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References
| Reference overview |
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| Clem, B. F., et al. 2013. Mol. Cancer Ther. 12, 1461. |
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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.
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