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Daporinad hydrochloride (FK 866 hydrochloride) is a potent nicotinamide-phosphate ribosyltransferase (NAMPT) inhibitor with potential anti-tumor and anti-angiogenic activity that induces apoptosis in tumor cells.Daporinad hydrochloride can be used in the study of inflammation and cancer.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $30 | In Stock | |
1 mL x 10 mM (in DMSO) | $78 | In Stock |
Description | Daporinad hydrochloride (FK 866 hydrochloride) is a potent nicotinamide-phosphate ribosyltransferase (NAMPT) inhibitor with potential anti-tumor and anti-angiogenic activity that induces apoptosis in tumor cells.Daporinad hydrochloride can be used in the study of inflammation and cancer. |
In vitro | METHODS: RPMI8226/S, U266 and MM1S cells were treated with FK866 (10nM, 24-48 hours) to study the effect of Nampt inhibitor on MAPK signaling pathway in MM cells. RESULTS: FK866 significantly reduced the gene and protein levels of pERK1/2, pp38MAPK and pSAPK/JNK, indicating that the drug has an effective inhibitory effect on MEK/ERK signaling. [1] |
In vivo | METHODS: CB17-SCID mice injected with MM1S cells were treated with FK866 (30 mg/kg, intraperitoneal injection, twice a day, for 4 days) once a week for 3 weeks. Caliper measurements of the longest perpendicular tumor diameter were taken twice a week, and excised tumors were collected from mice for Western blot analysis to assess ERK and LC3B phosphorylation. RESULTS: A significant reduction in tumor burden was observed on day 7 of FK866 treatment, the treatment was well tolerated, without significant weight loss or neurological changes, and resulted in a significant prolongation of overall survival; tumor tissues from FK866-treated mice showed a significant reduction in ERK phosphorylation and LC3 proteolytic cleavage. [1] |
Alias | FK 866 hydrochloride (658084-64-1 free base), FK 866 hydrochloride, APO866 |
Molecular Weight | 427.97 |
Formula | C24H30ClN3O2 |
Cas No. | 1785666-54-7 |
Smiles | Cl.O=C(C=CC=1C=NC=CC1)NCCCCC2CCN(C(=O)C=3C=CC=CC3)CC2 |
Relative Density. | 1.31g/cm3 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 10 mg/mL (23.37 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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