Биологическая активность
PQR514 is a мощный селективный pan-PI3K ингибитор with связывание Ki of 2.2 and 33 nM for p110α and mTOR, repectively.PQR514 inhibits phosphorylated S6 ribosomal protein (pS6, Ser235/236) and phosphorylation PKB Ser473 in A2058 cells с IC50 of 17 and 68 nM, respectively.PQR514 displays negligible interference with protein киназы activities at 10 uM in a KINOMEScan panel.PQR514 exhibits growth inhibition in vitro across a panel of 66 tumor cells with GI50 of 0.25 uM.PQR514 demonstrates significant antitumor activity aginst OVCAR-3 human ovarian cancer xenograft model in BALB/c nude mice.
Оригинал на английском
PQR514 is a potent selective pan-PI3K inhibitor with binding Ki of 2.2 and 33 nM for p110α and mTOR, repectively.PQR514 inhibits phosphorylated S6 ribosomal protein (pS6, Ser235/236) and phosphorylation PKB Ser473 in A2058 cells with IC50 of 17 and 68 nM, respectively.PQR514 displays negligible interference with protein kinase activities at 10 uM in a KINOMEScan panel.PQR514 exhibits growth inhibition in vitro across a panel of 66 tumor cells with GI50 of 0.25 uM.PQR514 demonstrates significant antitumor activity aginst OVCAR-3 human ovarian cancer xenograft model in BALB/c nude mice.
Химические свойства
- CAS №
- 1927857-55-3
- Брутто-формула
- C₁₆H₂₀F₂N₈O₂
- Мол. масса
- 394.38 г/моль
- SMILES
- C1(N)=NC=C(C2=NC(N3CCOCC3)=NC(N3CCOCC3)=N2)C(C(F)F)=N1
- Синонимы
- 2-Pyrimidinamine, 4-(difluoromethyl)-5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-
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.