Биологическая активность
DT2216-isomer is an isomer of DT2216. Compared to DT-2216, DT2216-isomer has a S-chiral carbon which links to the nitrogen atom of the aniline group. DT2216 is a мощный and селективный Bcl-xL-specific degrader. DT2216 is highly active against Bcl-xL-dependent T клетка lymphomas. DT2216 selectively killed various Bcl-xL-dependent TCL cells including MyLa cells in vitro. in vivo, DT2216 alone was highly effective against MyLa TCL xenografts in mice without causing significant thrombocytopenia or other toxicity. Furthermore, DT2216 combined with ABT199 (a селективный Bcl-2 ингибитор) synergistically reduced disease burden and improved survival in a TCL PDX mouse model dependent on both Bcl-2 and Bcl-xL.
Оригинал на английском
DT2216-isomer is an isomer of DT2216. Compared to DT-2216, DT2216-isomer has a S-chiral carbon which links to the nitrogen atom of the aniline group. DT2216 is a potent and selective Bcl-xL-specific degrader. DT2216 is highly active against Bcl-xL-dependent T cell lymphomas. DT2216 selectively killed various Bcl-xL-dependent TCL cells including MyLa cells in vitro. In vivo, DT2216 alone was highly effective against MyLa TCL xenografts in mice without causing significant thrombocytopenia or other toxicity. Furthermore, DT2216 combined with ABT199 (a selective Bcl-2 inhibitor) synergistically reduced disease burden and improved survival in a TCL PDX mouse model dependent on both Bcl-2 and Bcl-xL.
Химические свойства
- Брутто-формула
- C₇₇H₉₆ClF₃N₁₀O₁₀S₄
- Мол. масса
- 1,542.360 г/моль
- SMILES
- O=C([C@H]1N(C([C@@H](NC(CCCCCC(N2CCN(CC[C@H](NC3=CC=C(S(=O)(NC(C4=CC=C(N5CCN(CC6=C(C7=CC=C(Cl)C=C7)CCC(C)(C)C6)CC5)C=C4)=O)=O)C=C3S(=O)(C(F)(F)F)=O)CSC8=CC=CC=C8)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C9=CC=C(C%10=C(C)N=CS%10)C=C9)C
- Синонимы
- DT2216-isomer; DT 2216-isomer; DT-2216-isomer
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.