Linrodostat (Synonyms: BMS-986205; ONO-7701)
目录号: PL01244 纯度: ≥99%
CAS No. :1923833-60-6
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中文名称
Linrodostat
中文别名
顺式-(alphaR)-N-(4-氯苯基)-4-(6-氟-4-喹啉基)-alpha-甲基环己烷乙酰胺
英文名称
Linrodostat
英文别名
Linrodostat;BMS986205;(R)-N-(4-chlorophenyl)-2-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide;0A7729F42K;Linrodostat (USAN);(2R)-N-(4-chlorophenyl)-2-[cis-4-(6-fluoroquinolin-4-yl)cyclohexyl]propanamide;C24H24ClFN2O;GTPL9707;ONO 7701;BDBM50285416;NSC799771;s8629;BMS
Cas No.
1923833-60-6
分子式
C24H24ClFN2O
分子量
410.91
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Linrodostat (BMS-986205) 是一种选择性的不可逆的吲哚胺 2,3-双加氧酶 1 (IDO1) 抑制剂,对 IDO1-HEK293 细胞具有有效的抑制作用,其 IC50 值为1.1 nM。Linrodostat 在晚期癌症中具有良好的药理活性。
生物活性
Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC 50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers.
性状
Solid
IC50 & Target[1][2]
IDO1 1.1 nM (IC50)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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
溶解度数据
In Vitro: DMSO : 50 mg/mL (121.68 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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