TVB-3166 is a cell-permeable pyrrazole derivative that inhibits cellular palmitate synthesis (IC50 <100 nM) by fatty acid synthase (FASN) keto-reductase activity in a potent and reversible manner (IC50 = 42 nM), effectively inhibiting palmitate-dependent survival of various cancer cells in cultures and xenografted tumor growth in mice vivo (60-100 mg/kg/d p.o.), while exhibiting little or no anti-proliferation activity toward non-palmitate-dependent growth of cancer and non-cancer cultures. FASN inhibition by TVB-3166 treatment is also effective against the replications respiratory viruses both in cultures (Effc. conc. 200 nM against RSV and PIV3 in A549, HEp2, and HeLa cultures) and in mice (50 mg/kg/12 h, p.o.; RSV) in vivo without significant adverse effects to the host cells or mice.
| Molecular Weight | 384.47 |
| Formula | C24H24N4O |
| CAS Number | 1533438-83-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Nicols Montesdeoca, et al. Inhibitors of lipogenic enzymes as a potential therapy against cancer
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