Masofaniten (Androgen receptor-IN-2) is a potent and orally active androgen receptor inhibitor. Masofaniten inhibits androgen binding to androgen receptor with IC50 of 535 nM in the androgen-induced PSA-Luciferase assay.
Masofaniten inhibits cell proliferation in LNCaP and LNCaP95 cells with IC50 values of 0.44 μM and 3.78 μM respectively.
Masofaniten (60 mg/kg, p.o.) induces partial regressions of tumor growth in NCG mice bearing LNCaP tumors.
| Molecular Weight | 535.44 |
| Formula | C24H24Cl2N4O4S |
| CAS Number | 2416716-62-4 |
| Solubility (25°C) | DMSO 50 mg/mL (ultrasonic and warming) |
| Storage | -20°C, sealed |
| 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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