YM 511 is a orally active, potent aromatase (CYP19) inhibitor (IC50 values are 0.4 and 0.12 nM at rat ovary and human placenta cells respectively) that only weakly inhibits the synthesis of other steroid hormones. Reduces plasma estrogen levels into ranges induced by ovariectomy and inhibits testosterone-induced breast cancer cell growth in vitro (IC50 = 0.13 nM).
| Molecular Weight | 354.2 |
| Formula | C16H12BrN5 |
| CAS Number | 148869-05-0 |
| Solubility (25°C) | DMSO 35.42 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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