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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

仅限科研使用

Cat No : CM19253

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Synonyms

CPI 203|CPI-203

验证数据展示

  • CAS No.: 202591-23-9

    CPI203
    CAS#: 202591-23-9

产品信息

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
主要通路 表观遗传
分子量 399.9
纯度 99.71%， 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
别名 CPI 203|CPI-203

靶点活性

BET bromodomain:37 nM

体外活性

CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro. [1] CPI203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM, with low cytotoxicity in normal PBMCs from healthy donors. Furthermore, lenalidomide and CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells resistant to bortezomib. [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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