5MPN
Based on 3 publication(s) in Google Scholar
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines.
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- Reinheit: 99.89%
- CAS. Nr.: 47208-82-2
- Formel: C15H19N3O4
- Molecular Weight:305.33
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) 5MPN
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Biologische Aktivität
KI: 8.6 μM (PFKFB4)[1]
5MPN (0~30 μM; 24 hours; H460 cells) inhibits the expression of PFKFB4[1].
5MPN (0~50 μM; 0~72 hours; H460 NSCLC cells) first reduces the intracellular concentration of F2,6BP, glycolysis and ATP, which in turn results in a reduction in cell proliferation[1].
5MPN (0 and 10 μM; 6, 12 and 24 hours; H460 cells) induces cells apoptosis[1].
5MPN (0 and 10 μM; 6, 12 and 24 hours; H460 cells) arrests cell cycle progression[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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H460 cells
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Concentration:0~30 μΜ
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Incubation Time:24 hours
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Result:Inhibited the expression of PFKFB4 .
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Cell Line:H460 NSCLC cells
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Concentration:0~50 μM
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Incubation Time:0~72 hours
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Result:Resulted in a reduction in cell proliferation.
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Cell Line:H460 cells
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Concentration:0 and 10 μΜ
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Incubation Time:6, 12 and 24 hours
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Result:Induced cells apoptosis.
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Cell Line:H460 cells
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Concentration:0 and 10 μΜ
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Incubation Time:6, 12 and 24 hours
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Result:Arrested cell cycle progression.
5MPN causes a reduction in Ki67-positive cells in the LLC xenografts suggesting that 5MPN may be reducing cell cycle progression in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice[1]
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Dosage:120 mg/kg
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Administration:P.o.
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Result: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.
Chemical Information
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CAS. Nr. 47208-82-2
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Appearance Solid
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Molecular Weight 305.33
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Formel C15H19N3O4
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Color White to light yellow
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SMILES
COC1=C2N=CC=C(NCCCCCO[N+]([O-])=O)C2=CC=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
PFKFB4-Mediated HSPB1 phosphorylation suppresses ferroptosis to Promote gastric cancer progression. [Abstract]2026 Apr:246:117714. PMID: 41577048 -
Genes Genomics
Targeting phosphofructokinase 2 the isoform PFKFB4 suppresses glioblastoma proliferation and malignancy. [Abstract]2025 Oct 21. PMID: 41118116 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (327.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (642 KB)
- English - EN (642 KB)
- Français - FR (642 KB)
- Deutsch - DE (642 KB)
- Norwegian - NO (642 KB)
- Español - ES (642 KB)
- Swedish - SV (642 KB)
- Italian - IT (642 KB)
- Portuguese - PT (642 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.2751 mL | 16.3757 mL | 32.7515 mL | 81.8786 mL |
| 5 mM | 0.6550 mL | 3.2751 mL | 6.5503 mL | 16.3757 mL | |
| 10 mM | 0.3275 mL | 1.6376 mL | 3.2751 mL | 8.1879 mL | |
| 15 mM | 0.2183 mL | 1.0917 mL | 2.1834 mL | 5.4586 mL | |
| 20 mM | 0.1638 mL | 0.8188 mL | 1.6376 mL | 4.0939 mL | |
| 25 mM | 0.1310 mL | 0.6550 mL | 1.3101 mL | 3.2751 mL | |
| 30 mM | 0.1092 mL | 0.5459 mL | 1.0917 mL | 2.7293 mL | |
| 40 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0470 mL | |
| 50 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6376 mL | |
| 60 mM | 0.0546 mL | 0.2729 mL | 0.5459 mL | 1.3646 mL | |
| 80 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 mL | |
| 100 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL | 0.8188 mL |
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