Telaglenastat (CB-839) hydrochloride is a pioneering (first-in-class), selective, reversible, orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride has IC50 values of 23 nM and 28 nM for endogenous glutaminase in the kidney and brain of mice, respectively. Telaglenastat hydrochloride also induces autophagy and has strong antitumor activity.
| Molecular Weight | 608.04 |
| Formula | C26H25ClF3N7O3S |
| CAS Number | 1874231-60-3 |
| 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.
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