IPI-9119 is an orally active, selective and irreversible Fatty Acid Synthase (FASN) inhibitor, with an IC50 of 0.3 nM. IPI-9119 (0.05-5 μM; 6 days) significantly decreased AR-FL protein levels in AD LNCaP, AI C4-2 cells (expressing only AR-FL) and reduced the expression of AR-V7 in LNCaP-95, 22Rv1 AI cells.
In vivo, IPI-9119 (SC pump infusion; 0.5 μL/h; 100 mg/mL; for 28 days) inhibits tumor growth of CRPC xenografts mouse models.
| Molecular Weight | 495.43 |
| Formula | C24H19F2N5O5 |
| CAS Number | 1346564-56-4 |
| Solubility (25°C) | DMSO 90 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.
[3] Suzanne F Jones, et al. Clin Cancer Res. Molecular Pathways: Fatty Acid Synthase
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