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IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). IACS-10759 is orally bioavailable with excellent physicochemical properties in preclinical species and achieves significant in vivo efficacy with daily oral dosing of 10-25 mg/kg.
| 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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
| Molecular Weight | 562.56 |
| Formula | C25H25F3N6O4S |
| CAS Number | 1570496-34-2 |
| Purity | >99% |
| Solubility | DMSO ≥ 30 mg/mL |
| Storage | at -20°C |
IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities
Marina P, et al. AACR; Cancer Res. 2015 Aug;Volume 75, Issue 15 Supplement, pp. 4380.
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