GSK3179106 is an orally active, selective RET kinase inhibitor for human and rat RET IC50 0.4 nM and 0.2 nM, respectively. GSK3179106 has the potential for use in irritable bowel syndrome (IBS) by reducing post-inflammatory and stress-induced visceral hypersensitivity reactions.
| Molecular Weight | 467.41 |
| Formula | C22H21F4N3O4 |
| CAS Number | 1627856-64-7 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 60 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.
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Multi-kinase-IN-5 is a promising multi-kinase inhibitory agent. |
| NSC194598
NSC194598 is a p53 DNA-binding inhibitor with IC50 value of 180 nM and 2-40 μM for in vitro and in vivo, respectively. |
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