OM137 is an inhibitor of aurora kinases; inhibitor of spindle checkpoint. OM137 is an aminothiazole derivative, which functions to override the spindle checkpoint primarily through inhibition of the Aurora kinases (mitotic kinases). OM137 is a more potent inhibitor of Aurora B compared with Aurora A in vitro, consistent with the effects of OM137 on checkpoint function in living cells. The compound has some CDK1 inhibitory activity, but is likely that the major mode by which OM137 drives mitotic exit of cells arrested in M phase via the spindle checkpoint is through its inhibitory activity against Aurora B kinase. The compound is less potent than N-[4-[(6,7-Dimethoxy-4-quinazolinyl)amino]phenyl]benzamide hydrochloride (Sigma Cat. D6068), which is more suited for in vitro testing due to low solubility and high serum binding. OM137 is less potent than selective Aurora A inhibitor, cyclopropanecarboxylic acid {3-[4-(3-trifluoromethyl-phenylamino)-pyrimidin-2-ylamino]-phenyl}-amide (Sigma Cat. C2368).
| Molecular Weight | 306.34 |
| Formula | C13H14N4O3S |
| CAS Number | 292170-13-9 |
| Solubility (25°C) | DMSO: ≥10 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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