Ritlecitinib tosylate is a first-in-class, orally active, dual covalent inhibitor of tyrosine kinases in the JAK3 and TEC families. The IC50 for JAK3 is 33.1 nM and there is no activity against JAK1, JAK2 and TYK2.
| Molecular Weight | 457.55 |
| Formula | C22H27N5O4S |
| CAS Number | 2192215-81-7 |
| 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.
[1] No authors listed. Am J Health Syst Pharm. Ritlecitinib Tosylate
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| JAK2/FLT3-IN-1 TFA
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