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BAY885

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Chemical Structure| 2307249-33-6 同义名 : -
CAS号 : 2307249-33-6
货号 : A1176813
分子式 : C25H28F3N7O2
纯度 : 99%+
分子量 : 515.531
MDL号 : MFCD32067879
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(31.04 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 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.70mL

1.94mL

0.97mL

19.40mL

3.88mL

1.94mL
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