GSK872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with high affinity IC50 of 1.8 nM. GSK872 inhibits TNF- and virus-induced necrosis in 3T3-SA fibroblasts. It also inhibits necrosis induced by toll-like receptor 3 (TLR3). Pretreatment with GSK872 confers significant protection to primary hepatocytes.
| Molecular Weight | 383.49 |
| Formula | C19H17N3O2S2 |
| CAS Number | 1346546-69-7 |
| Solubility (25°C) | DMSO: ≥ 40 mg/mL |
| 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] Mandal P, et al. Mol Cell. RIP3 induces apoptosis independent of pronecrotic kinase activity.
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