Биологическая активность
PDE-I2 is a мощный and селективный ингибитор of malaria proliferation with Pf IC50 of 18 nM.PDE-I2 is a precursor of the anticancer duocarmycin family that preserves the class's sequence-specific DNA связывание but lacks its signature DNA alkylating cyclopropyl warhead.PDE-I2 retains comparable antimalarial potency to chloroquine.PDE-I2 is >1,000-fold less toxic to human клетка lines than duocarmycin, with mitigated impacts on eukaryotic chromosome stability.PDE-I2 treatment induces severe defects in parasite nuclear segregation leading to impaired daughter клетка formation during schizogony.
Оригинал на английском
PDE-I2 is a potent and selective inhibitor of malaria proliferation with Pf IC50 of 18 nM.PDE-I2 is a precursor of the anticancer duocarmycin family that preserves the class's sequence-specific DNA binding but lacks its signature DNA alkylating cyclopropyl warhead.PDE-I2 retains comparable antimalarial potency to chloroquine.PDE-I2 is >1,000-fold less toxic to human cell lines than duocarmycin, with mitigated impacts on eukaryotic chromosome stability.PDE-I2 treatment induces severe defects in parasite nuclear segregation leading to impaired daughter cell formation during schizogony.
Химические свойства
- CAS №
- 98296-23-2
- Брутто-формула
- C₂₅H₂₃N₅O₈
- Мол. масса
- 521.49 г/моль
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.