Биологическая активность
PD166326 is one of the most мощный members of the pyridopyrimidine class of protein tyrosine киназы inhibitors. In mice with the CML-like disease, PD166326 rapidly inhibited Bcr/Abl киназы activity after a single oral dose and demonstrated marked antileukemic activity in vivo. in vivo, PD166326 was also superior to imatinib mesylate in inhibiting the constitutive tyrosine phosphorylation of numerous leukemia-клетка proteins, including the src family member Lyn. PD166326 also prolonged the survival of mice with imatinib mesylate-resistant CML induced by the Bcr/Abl mutants P210/H396P and P210/M351T.
Оригинал на английском
PD166326 is one of the most potent members of the pyridopyrimidine class of protein tyrosine kinase inhibitors. In mice with the CML-like disease, PD166326 rapidly inhibited Bcr/Abl kinase activity after a single oral dose and demonstrated marked antileukemic activity in vivo. In vivo, PD166326 was also superior to imatinib mesylate in inhibiting the constitutive tyrosine phosphorylation of numerous leukemia-cell proteins, including the src family member Lyn. PD166326 also prolonged the survival of mice with imatinib mesylate-resistant CML induced by the Bcr/Abl mutants P210/H396P and P210/M351T.
Химические свойства
- CAS №
- 185039-91-2
- Брутто-формула
- C₂₁H₁₆Cl₂N₄O₂
- Мол. масса
- 427.28 г/моль
- SMILES
- O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=CC(CO)=C4)N=C3N1C
- Синонимы
- PD166326; PD166326; PD 166326.
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.