| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
KI: 8.6 μM (PFKFB4)[1]
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|---|---|
| ln Vitro |
5MPN (~30 μM; 24 hours; H460 cells) suppresses PFKFB4 expression[1]. Cell proliferation is subsequently inhibited by 5MPN (0~50 μM; 0~72 hours; H460 NSCLC cells), which first lowers the intracellular concentrations of F2,6BP, glycolysis, and ATP[1]. Cell apoptosis is induced by 5MPN (0 and 10 μM; 6, 12, and 24 hours; H460 cells)[1]. and 24 hours; H460 cells) halt the advancement of the cell cycle[1]. 5MPN (0.1, 1 or 10 µM) significantly inhibits PFKFB4 activity. 5MPN (H460 cells) leads to a dose-dependent decrease in the intracellular F2,6BP concentration. 5MPN (0~30 μM; over 48 hours; H460, H1299, H441, H522 and A549 cells) makes a dose-dependent reduction in cells growth. 5MPN (0~30 μM; 24 hours; H460 cells) inhibits PFKFB4 expression causing the observed reduction in H460 cell proliferation. 5MPN causes a G1 arrest in LLC cells in vitro similar to H460 cells[1].
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| ln Vivo |
5MPN (120 mg/kg; po) inhibits the growth of human lung adenocarcinoma xenografts H460 developed in athymic mice and Lewis lung carcinomas (LLC) grown in syngeneic animals without changing body weight[1]. Ki67-positive cells in the LLC xenografts decrease as a result of 5MPN, which may be preventing cell cycle progression in vivo[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: H460 cells Tested Concentrations: 0~30 μΜ Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited the expression of PFKFB4 . Cell Proliferation Assay[1] Cell Types: H460 NSCLC cells Tested Concentrations: 0~50 μM Incubation Duration: 0~72 hrs (hours) Experimental Results: Resulted in a reduction in cell proliferation. Apoptosis Analysis[1] Cell Types: H460 cells Tested Concentrations: 0 and 10 μM Incubation Duration: 6, 12 and 24 hrs (hours) Experimental Results: Induced cells apoptosis. Cell Cycle Analysis[1] Cell Types: H460 cells Tested Concentrations: 0 and 10 μM Incubation Duration: 6, 12 and 24 hrs (hours) Experimental Results: Arrested cell cycle progression. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 mice[1]
Doses: 120 mg/kg Route of Administration: Po Experimental Results: Suppressed the growth of Lewis lung carcinomas (LLC) grown in syngeneic mice and H460 human lung adenocarcinoma xenografts grown in athymic mice without affecting body weight. |
| References |
[1]. Chesney J, et al. Targeting the sugar metabolism of tumors with a first-in-class 6-phosphofructo-2-kinase (PFKFB4) inhibitor. Oncotarget. 2015;6(20):18001-18011.
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| Molecular Formula |
C15H19N3O4
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|---|---|
| Molecular Weight |
305.33
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| CAS # |
47208-82-2
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| SMILES |
O(CCCCCNC1C=CN=C2C(=CC=CC=12)OC)[N+](=O)[O-]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO: 100 mg/mL (327.51 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.19 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 25.0 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: ≥ 2.5 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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: ≥ 2.5 mg/mL (8.19 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: 20 mg/mL (65.50 mM) in Cremophor EL (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2751 mL | 16.3757 mL | 32.7514 mL | |
| 5 mM | 0.6550 mL | 3.2751 mL | 6.5503 mL | |
| 10 mM | 0.3275 mL | 1.6376 mL | 3.2751 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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