Биологическая активность
CQ627 is a targeted molecular glue that promotes RIOK2 degradation through the ubiquitin-proteasome pathway by bridging interactions between RIOK2 and the E3 ligase RNF126, achieving a DC50 of 410 nM in MOLT4 leukemia cells. This compound demonstrates multi-modal anticancer activity, including: (1) dose-dependent apoptosis induction, (2) G2/M phase клетка cycle arrest, and (3) broad-spectrum antiproliferative effects across cancer клетка lines. Furthermore, CQ627 shows significant in vivo efficacy in MOLT4 xenograft models, validating its therapeutic potential.
Оригинал на английском
CQ627 is a targeted molecular glue that promotes RIOK2 degradation through the ubiquitin-proteasome pathway by bridging interactions between RIOK2 and the E3 ligase RNF126, achieving a DC50 of 410 nM in MOLT4 leukemia cells. This compound demonstrates multi-modal anticancer activity, including: (1) dose-dependent apoptosis induction, (2) G2/M phase cell cycle arrest, and (3) broad-spectrum antiproliferative effects across cancer cell lines. Furthermore, CQ627 shows significant in vivo efficacy in MOLT4 xenograft models, validating its therapeutic potential.
Химические свойства
- Брутто-формула
- C₃₆H₂₇F₄N₇O₄
- Мол. масса
- 697.64 г/моль
- SMILES
- FC1=CC=C(C(/C=C/C(N2CCN(C3=C(C(F)(F)F)C=C(N4N=NC5=C4C6=CC(C7=CC=C(OC)N=C7)=CC=C6NC5=O)C=C3)CC2)=O)=O)C=C1
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.