|(2-氨基-4-(三氟甲氧基)苯基)(4-(7-(4-甲基哌嗪-1-基)吡啶并[3,2-d]嘧啶-4-基)哌啶-1-基)甲酮|CsnPharm

CAS No.: 2307249-33-6

BAY885 Catalog No. CSN27196

Synonyms: BAY885

BAY-885 is a highly potent and selective ERK5 inhibitor with IC50 value of 35nM.

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技术信息

生物活性

描述The extracellular signal-regulated kinase 5 (ERK5) is a member of the mitogen-activated protein kinase family. It acts as a key regulator of cellular signal transduction and can be activated by environmental stress, mitogens, and cytokines. BAY-885 is a potent and selective ERK5 inhibitor with an IC50 value of 35nM. It inhibited ERK5 transcription in SN12C-MEF2 reporter cell line with an IC50 value of 115nM and an IC90 value of 691nM. BAY-885 did not inhibit the proliferation of cells with ERK5 genomic amplification, including SN12C, SNU-449, and MFM-223 cell lines, or cells with constitutively active ERK5 signaling, such as BT-474 and SKBR-3 cell lines. BAY-885 is highly permeable in the Caco-assay. It exhibited no inhibition on the activity of CYP and hERG up to 20µM and 10µM, respectively. The metabolic stability of BAY-885 is low to moderate in rat hepatocytes and human liver microsomes^[1].
参考文献

[1] Nguyen D, Lemos C, Wortmann L, Eis K, Holton SJ, Boemer U, Moosmayer D, Eberspaecher U, Weiske J, Lechner C, Prechtl S, Suelzle D, Siegel F, Prinz F, Lesche R, Nicke B, Nowak-Reppel K, Himmel H, Mumberg D, von Nussbaum F, Nising CF, Bauser M, Haegebarth A. Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5. J Med Chem. 2019 Jan 24;62(2):928-940

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
- 1.9397 mL
- 9.6987 mL
- 19.3975 mL
- 5 mM
- 0.3879 mL
- 1.9397 mL
- 3.8795 mL
- 10 mM
- 0.1940 mL
- 0.9699 mL
- 1.9397 mL

技术信息

CAS号

2307249-33-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H28F3N7O2

运输

蓝冰

分子量

515.53

别名

BAY885

溶解度

DMSO	30.0 mg/mL (58.2 mM)
Water	Insoluble
Ethanol	8.0 mg/mL (15.5 mM)

动物实验配方

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