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Chemical Structure| 1923833-60-6 同义名 : BMS-986205;ONO-7701
CAS号 : 1923833-60-6
货号 : A883044
分子式 : C24H24ClFN2O
纯度 : 99%+
分子量 : 410.912
MDL号 : MFCD31729367
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(121.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Indoleamine 2,3-dioxygenase 1 (IDO1) is a cytosolic enzyme involved in immune metabolism and inflammatory programing via the regulation in tryptophan catabolism. BMS-986205 is a selective, irreversible inhibitor of IDO1 that potently inhibits kynurenine production in IDO1-HEK293 cells with an IC50 value of 1.1 nM[3]. BMS-986205 also displayed inhibitory effect on IDO1 in Hela cells with an IC50 value of 0.5 nM[4]. In IFNγ SKOV-3 cells, BMS-98620 exhibited 80% maximum inhibition on IDO1 activity with an IC50 value of 9.5nM. IDO1-mediated blockage of Jurkat T cell activation was rescued by BMS-986205 with an IC50 value of 8nM. Incubation with BMS-98620 for 72 hours also induced Jurkar cell death with an IC50 value of 6.3M[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.17mL

2.43mL

1.22mL

24.34mL

4.87mL

2.43mL
参考文献

[1]NCT02658890

[2]WO2016073770A1

[3]Abstract CT116: BMS-986205, an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic (PD) activity, alone and in combination with nivolumab (nivo) in advanced cancers in a phase 1/2a trial