EOAI3402143
目录号: PL01905 纯度: ≥99%
CAS No. :1699750-95-2
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中文名称
EOAI3402143
英文名称
EOAI3402143
英文别名
EOAI3402143 Tosylate;2-Cyano-3-(3,6-dichloro-pyridin-2-yl)-N-{1-[4-(2-morpholin-4-yl-ethoxy)-phenyl]-butyl}-acrylamide Tosylate;EOAI3402143
Cas No.
1699750-95-2
分子式
C32H36Cl2N4O6S
分子量
675.62
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
EOAI3402143 是一种去泛素化酶 (DUB) 抑制剂,抑制 Usp9x/Usp24 和 Usp5,这种作用存在剂量依赖性。
生物活性
EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.
性状
Solid
IC50 & Target[1][2]
Usp5
Usp9x
Usp24
体外研究(In Vitro)
EOAI3402143 retains potent Usp9x and Usp5 inhibitory activity. EOAI3402143 dose-dependently inhibits Usp9x and Usp24 activity, increases tumor cell apoptosis. Treatment of UM-2, UM-6, UM-16, and UM-76 with Usp9x inhibitor EOAI3402143 (G9) dose-dependently suppresses cell survival, while 600 nM of EOAI3402143 completely suppresses UM-2 3D colony growth when compared to untreated vehicle controls. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
To examine this potential, the effect of EOAI3402143 (G9) treatment is investigated on human MIAPACA2 tumor xenografts. Human MIAPACA2 cells are injected subcutaneously into NSG mice. Primary tumor development is monitored by caliper measurements, and once measurable, mice are separated into two groups and are treated with either vehicle control (PEG300/DMSO) or G9 at 15 mg/kg. Tumor growth, animal weight, behavior, and mobility are monitored during treatment. In parallel, murine 8041 tumors are also established and subjected to similar G9 treatment and tumor monitoring regimen as the human MIAPACA2 xenografts. Consistent with the in vitro findings, Usp9x inhibition results in the suppression of tumor growth in human tumor xenografts, but any significant effect on the growth of 8041 tumors xenografts is not observed, although the Usp9x activity is inhibited effectively by EOAI
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]. Potu H, et al. Usp5 links suppression of p53 and FAS levels in melanoma to the BRAF pathway. Oncotarget. 2014 Jul 30;5(14):5559-69.
[2]. Peterson LF, et al. Targeting deubiquitinase activity with a novel small-molecule inhibitor as therapy for B-cell malignancies. Blood. 2015 Jun 4;125(23):3588-97.
溶解度数据
In Vitro: DMSO : 50 mg/mL (99.32 mM; Need ultrasonic)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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