EOAI3402143

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Chemical Structure| 1699750-95-2 同义名 : -
CAS号 : 1699750-95-2
货号 : A1176706
分子式 : C25H28Cl2N4O3
纯度 : 99%+
分子量 : 503.421
MDL号 : MFCD31692368
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(99.32 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Ubiquitination plays an essential role in human cancers. EOAI3402143 is a deubiquitinase inhibitor that reduces the activity of deubiquitinase Usp5 and Usp9x in both vemurafenib sensitive and resistant A375 melanoma cells. Incubation of A375R cells with 2μM EOAI3402143 for 8 hours reduced the levels of pERK, pStat3, and increased the concentration of NOXA.[1] Treatment of pancreatic cancer patient-derived cell lines (UM-2, UM-6, UM-16, and UM-76) with EOAI3402143 (1-5μM) suppressed cell survival in a dose-dependently manner. EOAI3402143 at a concentration of 600nM completely suppressed UM-2 3D colony growth compared with the vehicle-treated controls. Treatment with 600nM EOAI3402143 also promoted the 3D colony growth of 8041 cells by two folds. In both human MIAPACA2 xenografts and mouse 8041 xenografts, administration with EOAI3402143 at 15mg/kg for 12 days effectively inhibited the activity of Usp9x in tumors. However, tumor suppression was only observed in human MIAPACA2 xenografts. [2] In NSH mice inoculated with A375 cells, treatment with EOAI3402143 at both 7.5 and 15mg/kg completely suppressed tumor growth.[1]
作用机制 EOAI3402143 is a small molecule deubiquitinase inhibitor that retains potent inhibitory activity against Usp5 and Usp9x.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.93mL

1.99mL

0.99mL

19.86mL

3.97mL

1.99mL
参考文献

[1]Potu H, Peterson LF, Pal A, Verhaegen M, Cao J, Talpaz M, Donato NJ. Usp5 links suppression of p53 and FAS levels in melanoma to the BRAF pathway. Oncotarget. 2014 Jul 30;5(14):5559-69. doi: 10.18632/oncotarget.2140

[2]Pal A, Dziubinski M, Di Magliano MP, Simeone DM, Owens S, Thomas D, Peterson L, Potu H, Talpaz M, Donato NJ. Usp9x Promotes Survival in Human Pancreatic Cancer and Its Inhibition Suppresses Pancreatic Ductal Adenocarcinoma In Vivo Tumor Growth. Neoplasia. 2018 Feb;20(2):152-164. doi: 10.1016/j.neo.2017.11.007