MRTX849 (Adagrasib) is a potent, highly selective, oral available KRAS G12C inhibitor. MRTX849 (Adagrasib) maximizes inhibition by irreversibly locking the KRAS molecule in its inactive state, thereby preventing tumor cell growth which results in tumor cell death. MRTX849 (Adagrasib) exhibited significantly improved half-life and penetration into the tumor, shutting down KRAS signaling for the entire dosing interval, and showing a higher degree of antitumor activity than previous KRAS mutant-selective inhibitors.
iScience. 2023 Jan 28;26(2):106080..
Global profiling of AMG510 modified proteins identified tumor suppressor KEAP1 as an off-target
MRTX849 (Adagrasib) purchased from AbMole
| Molecular Weight | 604.12 |
| Formula | C32H35ClFN7O2 |
| CAS Number | 2326521-71-3 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage | -20°C, dry, sealed |
| 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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