Биологическая активность
CFI-400945 is a мощный, highly селективный, orally available PLK4 ингибитор with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM; causes dysregulated centriole duplication, mitotic defects, and клетка death in multiple cancer клетка lines (A549 GI50=5 nM, OVCAR-3 GI50=18 nM); significantly inhibits human cancer xenografts; causes polyploidy, growth inhibition, and apoptotic death of murine and human lung cancer cells, despite expression of mutated KRAS or p53, produces supernumerary centrosomes and mitotic defects in lung cancer cells.
Оригинал на английском
CFI-400945 is a potent, highly selective, orally available PLK4 inhibitor with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM; causes dysregulated centriole duplication, mitotic defects, and cell death in multiple cancer cell lines (A549 GI50=5 nM, OVCAR-3 GI50=18 nM); significantly inhibits human cancer xenografts; causes polyploidy, growth inhibition, and apoptotic death of murine and human lung cancer cells, despite expression of mutated KRAS or p53, produces supernumerary centrosomes and mitotic defects in lung cancer cells.
Химические свойства
- CAS №
- 1616420-30-4
- Брутто-формула
- C₃₇H₃₈N₄O₇
- Мол. масса
- 650.73 г/моль
- SMILES
- O=C(C=CC(=O)O)O.O=C1NC2C=CC(OC)=CC=2C21CC2C1C=CC2C(=NNC=2C=1)C=CC1C=CC(CN2CC(C)OC(C)C2)=CC=1
- Синонимы
- CFI400945; CFI 400945
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.