Биологическая активность
Felezonexor, also known as CBS9106, SL-801, and BMS566419, is a novel reversible oral CRM1 ингибитор with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences. CBS9106 inhibits CRM1-dependent nuclear export, causing arrest of the клетка cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression. Oral administration of CBS9106 significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight.
Оригинал на английском
Felezonexor, also known as CBS9106, SL-801, and BMS566419, is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences. CBS9106 inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression. Oral administration of CBS9106 significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight.
Химические свойства
- CAS №
- 1076235-04-5
- Брутто-формула
- C₁₈H₂₁ClF₃N₃O₃
- Мол. масса
- 419.83 г/моль
- SMILES
- ClC1=C(C(F)(F)F)C([H])=C([H])C(=N1)N([H])N1C(C(C([H])([H])[H])=C(C1=O)C([H])([H])OC([H])([H])C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O
- Синонимы
- 1H-Pyrrole-2,5-dione, 1-[[6-chloro-5-(trifluoromethyl)-2-pyridinyl]amino]-3-[(3,3-dimethylbutoxy)methyl]-4-methyl-; PAW9EP9BXO; SB17170; 1-((6-Chloro-5-(trifluoromethyl)-2-pyridinyl)amino)-3-((3,3-dimethylbutoxy)methyl)-4-methyl-1H-pyrrole-2,5-dione; 1-[[6-Chloro-5-(trifluoromethyl)pyridin-2-yl]amino]-3-(3,3-dimethylbutoxymethyl)-4-methylpyrrole-2,5-dione
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 Publication: [1]. Sakakibara K, et al. CBS9106 is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. Blood. 2011 Oct 6;118(14):3922-31.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.