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CAS No.: 1446144-04-2

CPI-203 Catalog No. CSN16219

Synonyms: JQ-2;RG-6146;RO-6870810

CPI 203 is a potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bromodomain 4

IC50:~37nM
描述The Bromodomain and Extra-Terminal Domain BET (Bromodomain and Extra-Terminal Domain) family is characterized by the presence of two tandem bromodomains and an extra-terminal domain. BET proteins can govern the assembly of histone acetylation-dependent chromatin complexes, thus regulating gene expression. CPI-203, the JQ1 derivative, is the inhibitor of BET bromodomain with IC50 value of 37nM (measured by BRD4 α-screen assay). CPI203 can inhibit BRD4 in vitro and in cells. MYC mRNA can be suppressed after 4h exposure to CPI203 with IC50 value of 99nM in MV4-11 acute myelogenous leukemia (AML) cell line. Pre-incubation with CPI-203 for 2h can suppress IL-6 release stimulated by LPS for 16h in THP-1, with IC50 value of 30nM. CPI-203 did not affect BRD4 kinase activity in vitro kinase assays. In contrast, in cells, specific Ser2 phosphorylation by either endogenous BRD4 or exogenous BRD4 FEE-AAA can be markedly decreased by treatment with CPI-203 on concentration of 100-500nM^[1]. By inducing apoptosis and differentiation, RITA and CPI-203 synergize to drive CML CD34+ cell kill with combination indices (CIs) ranging from 0.07 to 0.34. Over 72h, combination of RITA with CPI-203 was also effective in synergistically eliminating residual CD34+CD38− cells (CI=0.3–0.8) in LSCs, suggesting the effect of RITA and CPI-203 on elimination of LSCs^[2]. CPI203 also showed synergistic antitumor activity of lenalidomide in bortezomib-resistant mantle cell lymphoma. Treatment with combination of CP203 (2.5mg/kg, BID) with lenalidomide (50mg/kg, daily) for 16 days reduction in tumor volume reached 62% in REC-1 xenografted SCID mice^[3].
作用机制CPI-203 can suppress BRD4-mediated Pol II CTD Ser2 phosphorylation by specific inhibition of BRD4 recruitment to chromatin. ^[1]
动物研究
剂量
Nude Mice (i.p.): 5 mg/kg Mice^[3] (i.p.): 2.5 mg/kg

给药途径
i.p.
参考文献

动物研究
剂量	Nude Mice (i.p.): 5 mg/kg Mice^[3] (i.p.): 2.5 mg/kg
给药途径	i.p.

[1] Devaiah BN, Lewis BA, et al. BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain. Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32.
[2] Abraham SA, Hopcroft LE, et al. Dual targeting of p53 and c-MYC selectively eliminates leukaemic stem cells. Nature. 2016 Jun 16;534(7607):341-6.
[3] Moros A, Rodr¨ªguez V, et al. Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma. Leukemia. 2014 Oct;28(10):2049-59

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5006 mL
- 12.5032 mL
- 25.0064 mL
- 5 mM
- 0.5001 mL
- 2.5006 mL
- 5.0013 mL
- 10 mM
- 0.2501 mL
- 1.2503 mL
- 2.5006 mL

技术信息

CAS号

1446144-04-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H18ClN5OS

运输

蓝冰

分子量

399.90

别名

JQ-2;RG-6146;RO-6870810

溶解度

DMSO	50.0 mg/mL (125.0 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+water	1 mg/mL	clear
PO	0.5% CMC-Na	30 mg/mL	suspension

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