AZ3146 is a novel Mps1 inhibitor with IC50 of 35 nM. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. AZ3146 displays selectivity over 46 other kinases including Cdk1 and aurora kinase B. AZ3146 also inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~15%, but its effect on Mad1 is less pronounced, with levels remaining at ~60%.
| Molecular Weight | 452.55 |
| Formula | C24H32N6O3 |
| CAS Number | 1124329-14-1 |
| Solubility (25°C) | DMSO 25 mg/mL Ethanol 90 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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