Empesertib (BAY1161909) is an orally bioavailable, selective inhibitor of the serine/threonine monopolar spindle 1 (Mps1) kinase (IC50 of < 1 nM), with potential antineoplastic activity. BAY1161909 also shows anti-tumor effect, suppressing the proliferation of Hela cells, with an IC50 of < 400 nM. The Mps1 kinase inhibitor Empesertib (BAY1161909) binds to and inhibits the activity of Mps1, it causes inactivation of the spindle assembly checkpoint (SAC), accelerated mitosis, chromosomal misalignment, chromosomal missegregation, mitotic checkpoint complex destabilization, and increased aneuploidy.
| Molecular Weight | 559.61 |
| Formula | C29H26FN5O4S |
| CAS Number | 1443763-60-7 |
| Solubility (25°C) | DMSO ≥ 24 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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