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CPI203

CPI203 (CPI 203) 是一种有效的 BET 溴结构域抑制剂（BRD4 的 IC50：37 nM）。

CAS号

202591-23-9

分子式

C19H18ClN5OS

主要靶点

Epigenetic Reader Domain|Others

仅限科研使用

Cat No : CM19253

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Synonyms

CPI-203|CPI203|CPI 203|BRD4|Epigenetic Reader Domain|EpigeneticReaderDomain

验证数据展示

  • CAS No.: 202591-23-9

    CPI203
    CAS#: 202591-23-9

产品信息

CPI203 (CPI 203) is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).

CAS号 202591-23-9
分子式 C19H18ClN5OS
主要靶点 Epigenetic Reader Domain|Others
主要通路 表观遗传
分子量 399.9
纯度 99.77%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
别名 CPI-203|CPI203|CPI 203|BRD4|Epigenetic Reader Domain|EpigeneticReaderDomain

靶点活性

BET BD:37 nM

体外活性

CPI203 在体外及细胞内抑制BRD4，而不影响其体外的激酶活性。[1] CPI203 在分析的所有9个MCL细胞系中显示出细胞静止效果，GI50范围从0.06到0.71 μM，对健康捐献者的正常PBMCs具有低细胞性毒性。此外，lenalidomide和CPI203通过靶向IRF4和MYC，有效激活对bortezomib有抵抗性的MCL细胞中的细胞死亡程序。[2]

溶解度

DMSO:200 mM

细胞实验

MCL primary cells and cell lines are incubated as indicated with lenalidomide and/or CPI203. MTT is added for 2-6 additional hours before spectrophotometric measurement. Each measurement is made in triplicate. Values are represented using untreated control cells. The GI50 is calculated as the concentration that produced 50 % growth inhibition. Combination indexes (CIs) are calculated by using the Calcusyn software version 2.0. The interaction between two drugs is considered synergistic when CI <1. (Only for Reference)

参考文献

1.Devaiah BN, et al. Proc Natl Acad Sci U S A. 2012, 109(18), 6927-6932.
2.Moros A, et al. Leukemia. 2014. doi: 10.1038/leu.2014.106.

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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