[CAS NO. 47208-82-2] 5MPN
PRODUCTS SPECIFICATIONS [47208-82-2]
DESCRIPTION [47208-82-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 305.33 |
| Molecular Formula | C15H19N3O4 |
| SMILES | COC1=C2N=CC=C(NCCCCCO[N+]([O-])=O)C2=CC=C1 |
Summary
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 ( K i =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 [1] .
IC50 & Target
KI: 8.6 μM (PFKFB4) [1]
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | H460 cells |
| Concentration: | 0~30 μΜ |
| Incubation Time: | 24 hours |
| Result: | Inhibited the expression of PFKFB4 . |
Cell Proliferation Assay [1]
| Cell Line: | H460 NSCLC cells |
| Concentration: | 0~50 μM |
| Incubation Time: | 0~72 hours |
| Result: | Resulted in a reduction in cell proliferation. |
Apoptosis Analysis [1]
| Cell Line: | H460 cells |
| Concentration: | 0 and 10 μΜ |
| Incubation Time: | 6, 12 and 24 hours |
| Result: | Induced cells apoptosis. |
Cell Cycle Analysis [1]
| Cell Line: | H460 cells |
| Concentration: | 0 and 10 μΜ |
| Incubation Time: | 6, 12 and 24 hours |
| Result: | Arrested cell cycle progression. |
In Vivo
5MPN (120 mg/kg; p.o.) suppresses 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
[1]
.
5MPN causes a reduction in Ki67-positive cells in the LLC xenografts suggesting that 5MPN may be reducing cell cycle progression in vivo
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57BL/6 mice [1] |
| Dosage: | 120 mg/kg |
| Administration: | P.o. |
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 327.51 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2751 mL | 16.3757 mL | 32.7515 mL |
| 5 mM | 0.6550 mL | 3.2751 mL | 6.5503 mL |
| 10 mM | 0.3275 mL | 1.6376 mL | 3.2751 mL |
-
1.
Add each solvent one by one: Cremophor EL
Solubility: 20 mg/mL (65.50 mM); Clear solution; Need ultrasonic
-
2.
-
3.
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
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution