CPI-203,1446144-04-2

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CPI-203

CAS No. : 1446144-04-2

MCE 国际站：CPI-203

产品活性：CPI-203 是一种有效的，选择性的，细胞通透的 BET bromodomain 抑制剂，抑制 BRD4，IC₅₀ 值约为 37 nM。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Epigenetic Reader Domain  |  Apoptosis

In Vitro: CPI-203 inhibits BRD4 in vitro and in cells, but does not affect BRD4 kinase activity in vitro. CPI-203 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, CPI-203 efficiently activates the cell death program in MCL cells.

In Vivo: CPI-203 (2.5 mg/kg, i.p.) combined with lenalidomide, enhances the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis in n REC-1 tumor-bearing mice.

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