Биологическая активность
H203 is a мощный dual Mdm2/MdmX ингибитор with Ki of 2/11 nM, respectively; H203 significantly reduced клетка viability in the cells overexpressing both Mdm2 and MdmX, and a significant and dose-dependent decrease in клетка number in H203-treated cells lacking Mdm2 or MdmX. H203-mediated decrease in клетка viability is strictly p53-dependent and H203 affects MdmX more specifically than nutlin-3a. H203 induced the expression of the p21 gene but not the p53 gene in treated cancer cells.
Оригинал на английском
H203 is a potent dual Mdm2/MdmX inhibitor with Ki of 2/11 nM, respectively; H203 significantly reduced cell viability in the cells overexpressing both Mdm2 and MdmX, and a significant and dose-dependent decrease in cell number in H203-treated cells lacking Mdm2 or MdmX. H203-mediated decrease in cell viability is strictly p53-dependent and H203 affects MdmX more specifically than nutlin-3a. H203 induced the expression of the p21 gene but not the p53 gene in treated cancer cells.
Химические свойства
- Брутто-формула
- C₃₅H₂₈Cl₂N₆O₄
- Мол. масса
- 667.55 г/моль
- Синонимы
- dual Mdm2/MdmX inhibitor H203
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.