|N-(3-(3-环丙基-5-((2-氟-4-碘苯基)氨基)-6,8-二甲基-2,4,7-三氧代-3,4,6,7-四氢吡啶并[4,3-d]嘧啶-1(2H)-基)苯基)乙酰胺二甲亚砜络合物|CsnPharm

CAS No.: 1187431-43-1

曲美替尼二甲基亚砜溶剂化物 Catalog No. CSN16943

Synonyms: GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate);GSK-1120212 DMSO Solvate

Trametinib DMSO Solvate is a specific MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MEK1

IC50:0.92nM MEK2

IC50:1.8nM
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.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01682083	Melanoma	Phase 3	Active, not recruiting	November 30, 2030	-
NCT01682083	-	-	Active, not recruiting	-	-
NCT01336634	Cancer	Phase 2	Active, not recruiting	December 1, 2020	-

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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.

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
- 1.4419 mL
- 7.2095 mL
- 14.4190 mL
- 5 mM
- 0.2884 mL
- 1.4419 mL
- 2.8838 mL
- 10 mM
- 0.1442 mL
- 0.7210 mL
- 1.4419 mL

技术信息

CAS号

1187431-43-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H29FIN5O5S

运输

蓝冰

分子量

693.53

别名

GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate);GSK-1120212 DMSO Solvate;Trametinib;JTP 74057;GSK-1120212;Trametinib dimethyl sulfoxide;JTP-74057 (DMSO solvate

溶解度

DMSO	67.0 mg/mL (96.6 mM) warming
Water	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01682083	Melanoma	Phase 3	Active, not recruiting	November 30, 2030	-
NCT01682083	-	-	Active, not recruiting	-	-
NCT01336634	Cancer	Phase 2	Active, not recruiting	December 1, 2020	-
NCT02416232	-	-	-	-	France ... more >> GSK Investigational Site Amiens Cedex, France, 80054 GSK Investigational Site Angers, France, 49100 GSK Investigational Site Bayonne cedex, France, 64109 GSK Investigational Site Besancon cedex, France, 25030 GSK Investigational Site Bobigny, France, 93000 GSK Investigational Site Bordeaux, France, 33075 GSK Investigational Site Boulogne-Billancourt, France, 92100 GSK Investigational Site Brest cedex, France, 29609 GSK Investigational Site Caen Cedex 9, France, 14033 GSK Investigational Site Chambray-Les-Tours, France, 37170 GSK Investigational Site Clermont-Ferrand cedex 1, France, 63003 GSK Investigational Site Creteil, France, 94010 GSK Investigational Site Dijon Cedex, France, 21079 GSK Investigational Site Grenoble cedex 9, France, 38043 GSK Investigational Site La Rochelle cedex 1, France, 17019 GSK Investigational Site Le Havre, France, 76083 GSK Investigational Site Le Mans, France, 72000 GSK Investigational Site Lille, France, 59037 GSK Investigational Site Limoges cedex, France, 87042 GSK Investigational Site Lorient, France, 56322 GSK Investigational Site Lyon Cedex 08, France, 69373 GSK Investigational Site Marseille Cedex 5, France, 13385 GSK Investigational Site Montpellier cedex 5, France, 34295 GSK Investigational Site Montpellier Cedex 5, France, 34298 GSK Investigational Site Mulhouse, France, 68100 GSK Investigational Site Nantes Cedex 1, France, 44093 GSK Investigational Site Nice, France, 06202 GSK Investigational Site Nimes, France, 30029 cedex 9 GSK Investigational Site Orleans Cedex 2, France, 45067 GSK Investigational Site Paris Cedex 10, France, 75475 GSK Investigational Site Paris, France, 75006 GSK Investigational Site Pau, France, 64000 GSK Investigational Site Pierre-Benite cedex, France, 69495 GSK Investigational Site Poitiers, France, 86021 GSK Investigational Site Pringy Cedex, France, 74374 GSK Investigational Site Reims Cedex, France, 51092 GSK Investigational Site Rennes Cedex, France, 35042 GSK Investigational Site Rouen, France, 76031 GSK Investigational Site Saint-Pierre, France, 97448 GSK Investigational Site Saint-Priest en Jarez, France, 42270 GSK Investigational Site Strasbourg Cedex, France, 67091 GSK Investigational Site Thionville, France, 57126 Cedex 1 GSK Investigational Site Toulouse Cedex 9, France, 31059 GSK Investigational Site Valence Cedex 9, France, 26953 GSK Investigational Site Vandoeuvre-Les-Nancy, France, 54511 GSK Investigational Site Villejuif cedex, France, 94805 Collapse <<
NCT02939846	Cancer	Phase 1	Withdrawn(Change in strategy)	December 2018	-
NCT02447939	Melanoma	Phase 1	Withdrawn(Change in strategy)	December 2018	-
NCT01336634	-	-	Active, not recruiting	-	-
NCT02083354	Cancer	Phase 2	Active, not recruiting	December 20, 2019	China, Guangdong ... more >> Novartis Investigative Site Guangzhou, Guangdong, China, 510060 China, Yunnan Novartis Investigative Site Kunming, Yunnan, China, 650106 China, Zhejiang Novartis Investigative Site Hangzhou, Zhejiang, China, 310022 China Novartis Investigative Site Beijing, China, 100036 Hong Kong Novartis Investigative Site Tuen Mun, Hong Kong Korea, Republic of Novartis Investigative Site Seoul, Korea, Republic of, 110-744 Novartis Investigative Site Seoul, Korea, Republic of, 120-752 Taiwan Novartis Investigative Site Kaohsiung, Taiwan, 807 Novartis Investigative Site Taipei, Taiwan, 100 Novartis Investigative Site Taoyuan County, Taiwan, 333 Thailand Novartis Investigative Site Bangkok, Thailand, 10320 Novartis Investigative Site Bangkok, Thailand, 10400 Novartis Investigative Site Songkla, Thailand, 90110 Collapse <<

靶点	Description	IC50
MEK1		IC50:0.92nM
MEK2		IC50:1.8nM

曲美替尼二甲基亚砜溶剂化物 Catalog No. CSN16943

靶点选择性

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