Биологическая активность
BMS-986365 (CC-94676) is a highly мощный and селективный AR degrader that induces rapid and deep degradation of both wildtype and mutant forms of the рецептор residing in either the cytoplasmic or nuclear compartments of the клетка. BMS-986365 (CC-94676) is about 100-fold more мощный than enzalutamide (ENZ) at inhibiting androgen-stimulated transcription of AR target genes, and 10 to 120-fold more мощный than ENZ at inhibiting AR-dependent proliferation of multiple prostate cancer клетка lines in vitro.
Оригинал на английском
BMS-986365 (CC-94676) is a highly potent and selective AR degrader that induces rapid and deep degradation of both wildtype and mutant forms of the receptor residing in either the cytoplasmic or nuclear compartments of the cell. BMS-986365 (CC-94676) is about 100-fold more potent than enzalutamide (ENZ) at inhibiting androgen-stimulated transcription of AR target genes, and 10 to 120-fold more potent than ENZ at inhibiting AR-dependent proliferation of multiple prostate cancer cell lines in vitro.
Химические свойства
- CAS №
- 2446928-30-7
- Брутто-формула
- C₄₁H₄₅F₃N₈O₅S
- Мол. масса
- 818.91 г/моль
- SMILES
- S=C1N(C2C=CC(C#N)=C(C(F)(F)F)C=2)C(C(C)(C)N1C1C=CC(=C(CC)C=1)OCCN1CCN(CC(NC2C=CC=C(C=2)NC2C(NC(CC2)=O)=O)=O)[C@H](C)C1)=O
- Синонимы
- SCHEMBL22128985; 2-[(2R)-4-[2-[4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-ethylphenoxy]ethyl]-2-methylpiperazin-1-yl]-N-[3-[(2,6-dioxopiperidin-3-yl)amino]phenyl]acetamide; YUVGVJYLOFTILT-NHYGQJMQSA-N
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.