Rineterkib hydrochloride (compound B) is an orally active inhibitor of ERK1/2 that exerts an antiproliferative effect by activating mutations in the MAPK pathway. Rineterkib hydrochloride can also inhibit RAF. This activity is particularly associated with KRAS-mutant non-small cell lung cancer, BRAF-mutant non-small cell lung cancer, KRAS-mutant pancreatic cancer, KRAS-mutant colon cancer, and KRAS mutant ovarian cancer.
| Molecular Weight | 614.89 |
| Formula | C26H28BrClF3N5O2 |
| CAS Number | 1715025-34-5 |
| Solubility (25°C) | DMSO ≥ 200 mg/mL |
| Storage | 4°C, protect from light, 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.
[3] No authors listed. Carteolol
[4] S HIFT, et al. Wien Med Wochenschr. [Prothipendyl-hydrochloride, a new neuroleptic]
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