Биологическая активность
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) ингибитор with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase клетка cycle arrest and клетка apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability.
Оригинал на английском
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability.
Химические свойства
- CAS №
- 2623158-64-3
- Брутто-формула
- C₁₉H₂₀F₃N₇
- Мол. масса
- 403.40 г/моль
- SMILES
- C1(C(NCC2C=CNN=2)=NC(NC2=CC=C3CN(C)CCC3=C2)=NC=1)C(F)(F)F
- Синонимы
- PCC0208017
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.