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Purity: ≥98%
PFK-015 (also known as PFK15) is a novel, potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM. PFK15 demonstrated cytotoxic effects on Jurkat and H522 lung adenocarcinoma cell lines, with IC50 values of 2.42 and 0.72 μM in Jurkat and H522, respectively. Moreover, PFK15 decreased intracellular ATP, glucose uptake, and F26BP, PFKFB3's substrate. PFK15 (3 μM) increased the number of cells undergoing early apoptosis in Jurkat T cell leukemia cells. In a dose-dependent manner, PFK15 (3 and 20 μM) increased the number of cells going through late apoptosis.
| Targets |
recombinant PFKFB3 (IC50 = 110 nM); PFKFB3 activity in cancer cells (IC50 = 20 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
For kinase reactions, 13 ng of recombinant human PFKFB3 protein is incubated for 1 hour at room temperature in a reaction mix that contains 10 μmol/L ATP, 10 μmol/L F6P, and either dimethyl sulfoxide (DMSO) vehicle control, 3PO, or PFK15. According to the manufacturer, kinase activity is determined using the Adapta Universal Kinase Assay.
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| Cell Assay |
Trypan blue exclusion is used to determine viability. For five minutes, the cells were incubated in 20% trypan blue. A standard hemocytometer is used to count all of the viable cells, excluding trypan blue cells. There are three duplicates of each experiment.
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| Animal Protocol |
C57Bl/6 mice bearing LLC xenografts, Balb/C athymic mice bearing CT26, U-87 MG, or BxPC-3 xenografts.
25 mg/kg every 3 days i.p. |
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| References |
| Molecular Formula |
C17H12N2O
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| Molecular Weight |
260.29
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| Exact Mass |
260.10
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| Elemental Analysis |
C, 78.44; H, 4.65; N, 10.76; O, 6.15
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| CAS # |
4382-63-2
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C2C(=C1)C=CC(=N2)/C=C/C(=O)C3=CC=NC=C3
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| InChi Key |
UJJUKZPBUMCSJZ-BQYQJAHWSA-N
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| InChi Code |
InChI=1S/C17H12N2O/c20-17(14-9-11-18-12-10-14)8-7-15-6-5-13-3-1-2-4-16(13)19-15/h1-12H/b8-7+
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| Chemical Name |
(E)-1-pyridin-4-yl-3-quinolin-2-ylprop-2-en-1-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (7.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2 mg/mL (7.68 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2 mg/mL (7.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO +45% PEG 300 +1% Tween 80 +ddH2O: 5mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8419 mL | 19.2093 mL | 38.4187 mL | |
| 5 mM | 0.7684 mL | 3.8419 mL | 7.6837 mL | |
| 10 mM | 0.3842 mL | 1.9209 mL | 3.8419 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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