BMS-986205

BMS-986205 (BMS-986205) 是一种选择性和不可逆的吲哚胺 2,3-双加氧酶 1 (IDO1) 抑制剂，在 IDO1-HEK293 细胞中的 IC50 值为 1.1 nM。 BMS-986205 在晚期癌症中具有良好的药效学活性。

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库存: 现货

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5mg

￥987.00

790.00

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10mg

￥1525.00

1220.00

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25mg

￥3050.00

2440.00

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50mg

￥4525.00

3620.00

- +

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货号: ajci22400
CAS: 1923833-60-6
别名: BMS-986205; ONO-7701
分子式: C24H24ClFN2O
分子量: 410.91
纯度: >98%
溶解度: DMSO : 50 mg/mL (121.68 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers[1][2].

Linrodostat (0.01-100 μM; 72 hours; SKOV-3 and Jurkat clone E6-1 cells) treatment reduces the number of viable cells compared with the non-treated control. Linrodostat also induces cell death at much lower concentrations and its IC50 is 6.3 μM[1].

参考文献:
[1]. Richards T, et al. Cell based functional assays for IDO1 inhibitor screening and characterization. Oncotarget. 2018 Jul 20;9(56):30814-30820.
[2]. Lillian L. Siu, et al. 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. AACR; Cancer Res. 2017; 77 (13 Suppl): Abstract nr CT116.