S87963 |
BMS-986205 |
MedMol | 98% |
- 产品描述: 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
- 靶点: IDO1:1.1 nM (IC50);IDO; Indoleamine2,3-Dioxygenase(IDO)
- 体外研究:
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. Cell Viability Assay Cell Line: SKOV-3 and Jurkat clone E6-1 cells Concentration: 0.01-100 μM Incubation Time: 72 hours Result: Reduced the number of viable cells compared with the non-treated control and induced cell death at much lower concentrations.
- 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.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.434 ml 12.168 ml 24.336 ml 5 mM 0.487 ml 2.434 ml 4.867 ml 10 mM 0.243 ml 1.217 ml 2.434 ml 50 mM 0.049 ml 0.243 ml 0.487 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)