Биологическая активность
TG-1701 (Edralbrutinib, TG1701) is a irreversible, orally available, мощный and highly specific BTK ингибитор with Kd of 3 nM, IC50 of 6.7 nM, more селективный than ibrutinib.TG-1701 exerts similar activity than the first-in-class BTKi ibrutinib, although with greater selectivity, in in vitro and in vivo models of B-NHL.TG-1701 impaired BCR downstream signaling in a concentration-dependent manner in IgM-stimulated cells, with maximal effects observed at 100 nM for TG-1701.TG-1701 shows mean GI50 of 6.4 uM in a set of 10 parental B-NHL клетка lines (MCL клетка lines GI50=4.3 uM).TG-1701 blunts Ikaros gene signature, including YES1 and MYC, in early-responder patients as well as in BTKi-sensitive B-NHL клетка lines and xenografts.
Оригинал на английском
TG-1701 (Edralbrutinib, TG1701) is a irreversible, orally available, potent and highly specific BTK inhibitor with Kd of 3 nM, IC50 of 6.7 nM, more selective than ibrutinib.TG-1701 exerts similar activity than the first-in-class BTKi ibrutinib, although with greater selectivity, in in vitro and in vivo models of B-NHL.TG-1701 impaired BCR downstream signaling in a concentration-dependent manner in IgM-stimulated cells, with maximal effects observed at 100 nM for TG-1701.TG-1701 shows mean GI50 of 6.4 uM in a set of 10 parental B-NHL cell lines (MCL cell lines GI50=4.3 uM).TG-1701 blunts Ikaros gene signature, including YES1 and MYC, in early-responder patients as well as in BTKi-sensitive B-NHL cell lines and xenografts.
Химические свойства
- CAS №
- 1858206-58-2
- Брутто-формула
- C₂₆H₂₃F₂N₅O₃
- Мол. масса
- 491.50 г/моль
- Синонимы
- TG1701, Edralbrutinib
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.