Molecular Formula | C19H19ClN6O2 |
Molar Mass | 398.8462 |
Density | 1.41±0.1 g/cm3(Predicted) |
Boling Point | 719.5±60.0 °C(Predicted) |
Solubility | DMSO: ≥ 44 mg/mL |
pKa | 11.10±0.10(Predicted) |
Storage Condition | -20℃ |
MDL | MFCD29472270 |
Physical and Chemical Properties | Bioactive Darolutamide (ODM-201, BAY-1841788) is a new androgen receptor (AR) antagonist, which can block AR nuclear transport with Ki of f 11 nM. Phase 3. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.507 ml | 12.536 ml | 25.072 ml |
5 mM | 0.501 ml | 2.507 ml | 5.014 ml |
10 mM | 0.251 ml | 1.254 ml | 2.507 ml |
5 mM | 0.05 ml | 0.251 ml | 0.501 ml |
target
Target Value
Androgen receptor 11 nM(Ki)
in vitro study
In AR-HEK293 cells that stably express full-length hAR, human AR (hAR) is ODM-201 inhibited, and the IC50 is 26 nM. ODM-201 inhibited VCaP cell proliferation, IC50 was 230 nM, but had no effect on the activity of the tested AR-negative cell lines, DU-145 prostate cancer cells and H1581 lung cancer cells.
in vivo studies
In mice loaded with VCaP xenografts, ODM-201 (50 mg/kg, p.o.) significantly inhibited the growth of castration-resistant prostate tumors.