Биологическая активность
BMS-986202 (BMS 986202) is мощный, селективный Tyk2 ингибитор that binds to Tyk2 JH2 domain с IC50 of 0.19 nM, Ki of 0.02 nM, >10,000-fold over 273 kinases and pseudokinases; BMS-986202 demonstrated клеточный activity (IL-23 IC50=12 nM) in IL-23 stimulated reporter assay (in Kit225 T cells). BMS-986202 also binds Jak1 JH2 with an IC50 of 7.8 nM, but this enzymatic связывание did not lead to any functional activities, as BMS-986202 displayed an activity (IC50) of greater than 12.5 μM in the IL-2 stimulated Jak1/3-dependent клеточный assay. BMS-986202 showed in vivo efficacy in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.
Оригинал на английском
BMS-986202 (BMS 986202) is potent, selective Tyk2 inhibitor that binds to Tyk2 JH2 domain with IC50 of 0.19 nM, Ki of 0.02 nM, >10,000-fold over 273 kinases and pseudokinases; BMS-986202 demonstrated cellular activity (IL-23 IC50=12 nM) in IL-23 stimulated reporter assay (in Kit225 T cells). BMS-986202 also binds Jak1 JH2 with an IC50 of 7.8 nM, but this enzymatic binding did not lead to any functional activities, as BMS-986202 displayed an activity (IC50) of greater than 12.5 μM in the IL-2 stimulated Jak1/3-dependent cellular assay. BMS-986202 showed in vivo efficacy in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.
Химические свойства
- CAS №
- 1771691-34-9
- Брутто-формула
- C₂₂H₂₁FN₆O₃
- Мол. масса
- 439.46 г/моль
- SMILES
- FC1C([H])=NC(C2C([H])=C([H])C([H])=C(C=2OC([H])([H])[H])N([H])C2C(C(N([H])C([2H])([2H])[2H])=O)=C([H])N=C(C=2[H])N([H])C(C2([H])C([H])([H])C2([H])[H])=O)=NC=1[H]
- Синонимы
- BMS-986202; J2Q5XQZ64C; BDBM50565986; BMS986202; 3-Pyridinecarboxamide, 6-((cyclopropylcarbonyl)amino)-4-((3-(5-fluoro-2-pyrimidinyl)-2-methoxyphenyl)amino)-N-(methyl-d3)- и ещё 2
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.