Forodesine hydrochloride is a potent and orally active transition-state analog inhibitor of purine nucleoside phosphorylase. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels, acts as a potent human lymphocyte proliferation inhibitor.
At a single dose of 10 mg/kg in mice, Forodesine elevates dGuo to approximately 5 μM. In the human peripheral blood lymphocyte severe combined immunodeficiency (hu-PBL-SCID) mouse model, Forodesine is effective in prolonging the life span 2-fold or more.
| Molecular Weight | 302.71 |
| Formula | C11H15ClN4O4 |
| CAS Number | 284490-13-7 |
| Form | Solid |
| Solubility (25°C) | Water 15 mg/mL DMSO 9 mg/mL |
| Storage | -20°C, 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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