GlpBio

BET bromodomain inhibitor

目录号: GC16299纯度: >99.50%同义词: BET抑制剂,CPI-0610; CPI0610; CPI 0610
BET 溴结构域抑制剂是从专利 WO/2015/153871A2 化合物实施例 11 中提取的一种有效的 BET 抑制剂。
BET bromodomain inhibitor
Cas No.: 1380087-89-7
规格价格库存数量操作
10mg¥1,620.00现货
1
50mg¥5,580.00现货
1
10mM (in 1mL DMSO)¥972.00现货
1
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文献被引

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产品描述 Description

IC50: < 500 nM for BRD4

BET (bromodomain and extra-terminal) proteins regulate gene expression through their ability to bind to acetylated chromatin and subsequently activate RNA PolII-driven transcriptional elongation. The bromodomain (BRD) and extra-C terminal domain (BET) protein family consists of four members (BRD2, BRD3, BRD4 and BRDT).Small molecule BET inhibitors prevent binding of BET proteins to acetylated histones and inhibit transcriptional activation of BET target genes. BET inhibitors attenuate cell growth and survival in several hematologic cancer models, partially through the down-regulation of the critical oncogene, MYC. BET bromodomain inhibitor is a potent and selective inhibitor for BRD4.

In vitro: The most potent systhsized ompound presented is BET bromodomain inhibitor, which shows activity with IC50 < 500 nM against BRD4 [1].

In vivo: BET bromodomain inhibitor shows activity in vivo at < 10 mg/kg against BRD4 in rat [1].

Clinical trial: Up to now, BET bromodomain inhibitor is still in the preclinical development stage.

Reference:
[1] Garnier JM, Sharp PP, Burns CJ.  BET bromodomain inhibitors: a patent review. Expert Opin Ther Pat. 2014 Feb;24(2):185-99.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Primary Multiple Myeloma cell lines

Preparation method

The solubility of this compound in DMSO is >18.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

2 μM at 72 h

Applications

CPI-0610 treatment resulted in 40% decrease in viability in primary cells isolated from a newly diagnosed patient and caused 50% cell death in primary cells isolated from a relapsed disease patient.
Animal experiment [1]:

Animal models

Multiple Myeloma xenograft CB17-SCID mouse model

Dosage form

subcutaneous injections, 10 mg/kg, twice a day for 38 days

Application

Mice treated with CPI-0610 showed a significant delay in tumor growth, and the median overall survival of CPI-0610 treated animals was significantly prolonged.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Siu KT, Ramachandran J, Yee AJ, et al. Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma. Leukemia. 2017 Jan 3.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1380087-89-7
同义词
BET抑制剂,CPI-0610; CPI0610; CPI 0610
化学名
2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetimidic acid
SMILES
CC1=NOC2=C1C3=CC=CC=C3C(C4=CC=C(Cl)C=C4)=N[C@@]2([H])CC(O)=N
分子式
C20H16ClN3O2
分子量
365.81 g/mol
溶解性
≥ 18.3mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol