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%.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 25 mg/mL
Ethanol 90 mg/mL
Mps1 directs the assembly of Cdc20 inhibitory complexes during interphase and mitosis to control M phase timing and spindle checkpoint signaling.
Maciejowski J, et al. J Cell Biol. 2010 Jul 12;190(1):89-100. PMID: 20624902.
Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex.
Hewitt L, et al. J Cell Biol. 2010 Jul 12;190(1):25-34. PMID: 20624899.
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