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CAS No.: 263707-16-0

ESI-09 Catalog No. CSN18168

Synonyms: ESI-09

ESI-09 is selective inhibitor of EPAC1 and EPAC2 with IC50 of 3.2 μM and 1.4 μM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 value of 1.4μM for inhibition of cAMP-mediated EPAC2 GEF activity. ESI-09 inhibited EPAC- but not EGF-mediated Akt phosphorylation induced by 007-AM in AsPC-1 pancreatic cancer cells at 1 and 10μM. Also, it inhibited EPAC2-mediated insulin secretion in INS-1 cells at 10μM. Inhibition of EPAC1by ESI-09 at 10μM for 24h decreased pancreatic cancer cell, AsPC-1 and PANC-1, migration and invasion. A dose-dependent inhibition of EPAC1-mediated adhesion of PDA cells on collagen I could be observed post treatment with ESI-09 at concentration ranging in 1-10μM.
作用机制ESI-09 can competitively bind to EPAC.^[1]
动物研究
剂量
Rat: 1 mg/kg^[2] (i.p.)
Mice: 10 mg/kg^[3] (i.p.); 50 mg/kg^[3] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Rat: 1 mg/kg^[2] (i.p.) Mice: 10 mg/kg^[3] (i.p.); 50 mg/kg^[3] (p.o.)
给药途径	i.p., p.o.

[1] Almahariq M, Tsalkova T, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol. 2013 Jan;83(1):122-8.

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
- 3.0233 mL
- 15.1163 mL
- 30.2326 mL
- 5 mM
- 0.6047 mL
- 3.0233 mL
- 6.0465 mL
- 10 mM
- 0.3023 mL
- 1.5116 mL
- 3.0233 mL

技术信息

CAS号

263707-16-0

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H15ClN4O2

运输

蓝冰

分子量

330.77

别名

ESI-09

溶解度

DMSO	330.0 mg/mL (997.7 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	3.3 mg/mL	clear
PO	0.5% CMC-Na	43 mg/mL	suspension

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ESI-09 Catalog No. CSN18168

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