Trametinib (DMSO solvate)

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Chemical Structure| 1187431-43-1 同义名 : GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate);Trametinib dimethyl sulfoxide;JTP-74057;GSK1120212;Trametinib DMSO solvate
CAS号 : 1187431-43-1
货号 : A286366
分子式 : C28H29FIN5O5S
纯度 : 98%
分子量 : 693.528
MDL号 : MFCD21609250
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

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

DMSO: 3 mg/mL(4.33 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 Trametinib DMSO Solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.44mL

0.29mL

0.14mL

7.21mL

1.44mL

0.72mL

14.42mL

2.88mL

1.44mL
参考文献

[1]Yamaguchi T, Kakefuda R, et al. Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with leflunomide. Inflamm Res. 2012 May;61(5):445-54.

[2]Yamaguchi T, Kakefuda R, et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol, 2011, 39(1), 23-31.