Zasocitinib (NDI-034858) is a highly selective, orally active TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM. Zasocitinib inhibits phosphorylation induction of heterodimer complex Tyk2 /JAK2-mediated IL-12 (1.7 ng/mL) effect, with IC50 value of <0.1 μM in human peripheral blood mononuclear cell.
| Molecular Weight | 460.49 |
| Formula | C23H24N8O3 |
| CAS Number | 2272904-53-5 |
| 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.
[3] Sohita Dhillon. Drugs. Tofacitinib: A Review in Rheumatoid Arthritis
[5] Omer Ibrahim, et al. JAMA Dermatol. Treatment of Alopecia Areata With Tofacitinib
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JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. |
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