Metarrestin (ML246) is a first-in-class, oral active and specific perinucleolar compartment (PNC) inhibitor. It can destroy the nucleolus structure and inhibit the transcription of RNA polymerase (Pol) I. Metarrestin blocks the development of metastasis and prolongs survival in mouse cancer models.
Molecular Weight | 474.6 |
Formula | C31H30N4O |
CAS Number | 1443414-10-5 |
Solubility (25°C) | DMSO:21 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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