Биологическая активность
SB02024 is a novel highly мощный, селективный, ATP competitive, orally active ингибитор of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times селективный towards other PI3K isoenzymes; SB02024 is also highly селективный at 1 uM in the DiscoveRx ScanMax panel of 468 kinases; reduces the number of GFP-2xFYVE puncta с IC50 of 14 nM, induces a dose-dependent increase in levels of NCOA4 and p62; blocks autophagy in vitro and reduces xenograft growth of two breast cancer клетка lines, MDA-MB-231 and MCF-7; also significantly potentiates cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro.
Оригинал на английском
SB02024 is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes; SB02024 is also highly selective at 1 uM in the DiscoveRx ScanMax panel of 468 kinases; reduces the number of GFP-2xFYVE puncta with IC50 of 14 nM, induces a dose-dependent increase in levels of NCOA4 and p62; blocks autophagy in vitro and reduces xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7; also significantly potentiates cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro.
Химические свойства
- CAS №
- 2126737-28-6
- Брутто-формула
- C₁₆H₂₂F₃N₃O₂
- Мол. масса
- 345.36 г/моль
- SMILES
- O=C1NC(N2[C@@H](C(F)(F)F)CCCC2)=CC(N3[C@H](C)COCC3)=C1
- Синонимы
- SB02024; SB-02024; SB 02024
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 Publication: 1. Dyczynski M, et al. Cancer Lett. 2018 Jul 25. pii: S0304-3835(18)30486-5.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.