|4-(2-溴-6-氟苯甲酰基)-N-(吡啶-3-基)-1H-吡咯-2-甲酰胺|CsnPharm

CAS No.: 1888305-96-1

ERK5-IN-2 Catalog No. CSN24288

Synonyms: ERK5-IN-2

ERK5-IN-2 is a selective ERK5 inhibitor with IC50 value of 0.82 μM.

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技术信息

生物活性

描述Extracellular signal-regulated kinase 5 (ERK5), a member of the mitogen-activated protein kinase (MAPK) family, is ubiquitously expressed in mammalian tissues and cell types, where it is activated by extracellular stimuli, including several growth factors and cellular stresses^[1]. ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC₅₀s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively^[2]. An anti-angiogenic effect was apparent with Matrigel plugs from mice treated with ERK5-IN-2 (100 mg/kg, p.o.) twice daily for 7 days^[2]. In a human tumour xenograft model (A2780 cells), ERK5-IN-2 (100 mg/kg, p.o.) treatment twice-daily for 10 days led to significant tumour volume reduction by 57% when compared to the control group^[2].
作用机制ERK5-IN-2 binds in the ERK5 ATP-binding site.
参考文献

[1] Stecca B, Rovida E. Impact of ERK5 on the Hallmarks of Cancer. Int J Mol Sci. 2019 Mar 21;20(6):1426. doi: 10.3390/ijms20061426. PMID: 30901834; PMCID: PMC6471124.
[2] Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang LZ, Wong AC, Noble MEM, Wedge SR, Cano C. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4. Eur J Med Chem. 2019 Sep 15;178:530-543. doi: 10.1016/j.ejmech.2019.05.057. Epub 2019 May 25. PMID: 31212132.

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
- 2.5761 mL
- 12.8803 mL
- 25.7605 mL
- 5 mM
- 0.5152 mL
- 2.5761 mL
- 5.1521 mL
- 10 mM
- 0.2576 mL
- 1.2880 mL
- 2.5761 mL

技术信息

CAS号

1888305-96-1

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H11BrFN3O2

运输

蓝冰

分子量

388.19

别名

ERK5-IN-2

溶解度

DMSO	78.0 mg/mL (200.9 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (7.7 mM)

动物实验配方

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