现货,GSK1120212 (JTP-74057) ,CAS号: 871700-17-3,美国进口, MAPK , MEK , MEK 抑制剂,selleck,S2637

信号转导通路: MAPK >> MEK >> MEK 抑制剂 >> GSK1120212 (JTP-74057)http://selleck.cn/gsk1120212-jtp-74057-S2673.html

技术数据:

分子量(MW): 615.39

化学式:

C26H23FIN5O4

 

溶解度: DMSO ≥6mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 871700-17-3

生物活性

 

 

GSK1120212 (JTP-74057) is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2. [1] GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases. After treatment of GSK1120212 (JTP-74057), it led to the growth inhibition and upregulate p15INK4b and/or p27KIP1 in most of the colorectal cancer cell lines tested. In nude animal mice studies, JTP-74057 inhibited tumor growth of HT-29 and COLO205 xenografts when GSK1120212 (JTP-74057) was daily oral administered for 14 days. GSK1120212 (JTP-74057) showed an additive or a synergistic action in combination with the standard-of-care agents, 5-fluorouracil, oxaliplatin or SN-38. Sensitivity to JTP-74057-induced apoptosis may be an important factor for the estimation of in vivo efficacy, and sensitivity was enhanced by an Akt inhibitor. [2] GSK1120212 (JTP-74057) is originally developed by GlaxoSmithKline and is recruiting for phase I clinical trials for the treatment of solid tumors.

 

 

 

参考文献

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

GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Gilmartin AG et al. Clin Cancer Res. 2011 Mar 1;17(5):989-1000.

客户反馈数据

如果需要长期保存,请于零下二十度低温保存。

禁止用于人体及治疗!

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