Nafamostat Mesylate(FUT-175) (Synonyms: Coahibitor, FUT 175, Nafamastat)

Cell lines

The human pancreatic tumor cell lines PANC-1

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

3 h; 160 μg/mL

Applications

In assessment of the NF- κB activation by ELISA, concentration of NF- κB p65 in the nuclear extracts of PANC-1 cells in combination group was statistically lower than those in oxaliplatin group (p<0.0001). Like nuclear NF-κB levels, phosphorylated IκBa levels by Western blot analysis in combination group were significantly lower than those in oxaliplatin group (p=0.037). In other words, FUT-175 inhibits oxaliplatin-induced NF- κB activation by suppressing IκBa phosphorylation in vitro.

Animal models

Five-week-old male nude mice

Dosage form

30 μg/g; thrice a week for 6 weeks; intraperitoneal injection

Applications

A pancreatic cancer model was established by injection of PANC-1 cells (5×10-6cells) in 200 μM of PBS subcutaneously into the right side of the back of the animals. In vivo, the tumor growth in combination group (oxaliplatin and nafamostat mesilate) was significantly slower than that of oxaliplatin group (p<0.0001). Tumor volume in combination group was significantly smaller than that of oxaliplatin group (p=0.048).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Gocho T, Uwagawa T, Furukawa K, et al. Combination chemotherapy of serine protease inhibitor nafamostat mesilate with oxaliplatin targeting NF-κB activation for pancreatic cancer[J]. Cancer letters, 2013, 333(1): 89-95.