| Identification | Back Directory | [Name]
5-(N-(8-METHOXY-4-QUINOLYL)AMINO)PENTYL NITRATE | [CAS]
47208-82-2 | [Synonyms]
PFKFB4 inhibitor 5MPN
5-(N-(8-METHOXY-4-QUINOLYL)AMINO)PENTYL NITRATE
1-Pentanol, 5-[(8-methoxy-4-quinolinyl)amino]-, 1-nitrate | [Molecular Formula]
C15H19N3O4 | [MDL Number]
MFCD00089445 | [MOL File]
47208-82-2.mol | [Molecular Weight]
305.33 |
| Chemical Properties | Back Directory | [Boiling point ]
493.8±40.0 °C(Predicted) | [density ]
1.244±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
6.36±0.50(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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]. | 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.
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| [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. DOI:10.18632/oncotarget.4534 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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