Биологическая активность
RIOK2-IN-1 (com 4) is a мощный and селективный RIOK2 ингибитор (Kd=150 nM), but has low клеточный activity (IC50=14,600 nM). RIOK2 is an atypical киназы associated with a variety of human cancers and is involved in ribosome maturation and клетка cycle progression. The малая молекула ингибитор CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression.
Оригинал на английском
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression.
Химические свойства
- CAS №
- 1088216-72-1
- Брутто-формула
- C₁₈H₁₆N₂O
- Мол. масса
- 276.33 г/моль
- SMILES
- O=C(CC1=CC2=C(C=CC=C2)C=C1)NC3=NC=CC(C)=C3
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.