CPI-203
目录号: PL13475 纯度: ≥98%
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。
CAS No. :1446144-04-2
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中文名称
CPI-203
中文别名
6-氟-2,4-二溴-3-羟基吡啶;CPI-203 抑制剂
英文名称
CPI-203
英文别名
CPI 203;CPI-203;6H-​Thieno[3,​2-​f]​[1,​2,​4]​triazolo[4,​3-​a]​[1,​4]​diazepine-​6-​acetamide, 4-​(4-​chlorophenyl)​-​2,​3,​9-​trimethyl-​, (6S)​-;(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide;CPI203;C19H18ClN5OS;(s)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide;GTPL7513;AOB6784;s7304;2338AH;SB19335;CPI203, >=98% (HPLC);BC600523;SW219296-1;8-{(1S)-1-[8-(Triflu;2-[(9S)-7-(4-Chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6)
Cas No.
1446144-04-2
分子式
C19H18ClN5Os
分子量
399.90
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC 50 value of appr 37 nM (BRD4 α-screen assay).
性状
Solid
IC50 & Target[1][2]
IC50: 37 nM (BRD4)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
参考文献
[1]. Devaiah BN, 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]. Moros A, 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
溶解度数据
In Vitro: DMSO : ≥ 47 mg/mL (117.53 mM)配制储备液
搜索质检报告(COA)

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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