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GSK126

GSK126 更多供应商
公司名称:上海瀚香生物科技有限公司  黄金产品
联系电话:+86 15971444841
产品介绍:英文名称:GSK126
CAS:1346574-57-9
纯度:98% 包装信息:mg;g
公司名称:上海楼岚生物科技有限公司  黄金产品
联系电话:+86-21-61128122
产品介绍:英文名称:GSK126
CAS:1346574-57-9
公司名称:上海波以尔化工有限公司  
联系电话:86-15221043597
产品介绍:英文名称:S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide
CAS:1346574-57-9
公司名称:百灵威科技有限公司  
联系电话:400-666-7788 +86-10-82848833
产品介绍:英文名称:GSK126
CAS:1346574-57-9
包装信息:1Mg,50Mg,5Mg 备注:化学试剂、精细化学品、医药中间体、材料中间体
公司名称:凯试(上海)科技有限公司  
联系电话:021-50135380
产品介绍:英文名称:GSK126
CAS:1346574-57-9
纯度:98% 备注:1620元/1mg; 2900元/5mg; 18000元/50mg
GSK126
生物活性 体外研究 体内研究
中文名称:GSK126
中文同义词:GSK126;GSK126;GSK-126;GSK 126;CPDB1065
英文名称:S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide
英文同义词:S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide;N-[(4,6-Dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-((1S)-1-methylpropyl)-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide;1-(S)-sec-butyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide;GSK 126 N-[(4,6-Dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-((1S)-1-methylpropyl)-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide;N-[(4,6-Dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-((1S)-1-methylpropyl)-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide GSK126;GSK126, >=98%;N-[(4,6-Dimethyl-2-ox;GSK-2816126
CAS号:1346574-57-9
分子式:C31H38N6O2
分子量:526.67242
EINECS号:-0
相关类别:信号转导通路激酶抑制剂;细胞周期;API;小分子抑制剂;Inhibitors;小分子抑制剂,天然产物
Mol文件:1346574-57-9.mol
GSK126
GSK126 性质
GSK126 用途与合成方法
生物活性GSK126 是一种有效的,高选择性EZH2 methyltransferase抑制剂,IC50为9.9 nM,对 EZH2 的选择性比其他20种人甲基转移酶高1000多倍。
体外研究GSK126 induced a 50% loss of H3K27 tri-methylation (H3K27me3) in both EZH2 wild-type and mutant DLBCL cell lines at concentrations ranging from 7–252 nM independent of EZH2 mutation status. GSK126 suppresses cell proliferation of a panel of B-cell lymphoma cell lines. Six of the seven most sensitive DLBCL cell lines harboured Y641N, Y641F or A677G EZH2 mutations (growth IC50 = 28–861  nM). 72 h treatment with 500 nM GSK126 induces transcriptional activation in sensitive cell lines.
体内研究GSK126 treated once-daily for 10 days decreases global H3K27me3 and increases gene expression in subcutaneous xenografts of KARPAS-422 in a dose-dependent fashion. With daily 50 mg per kg dosing, complete tumour growth inhibition is observed. When higher dosing regimens are examined with KARPAS-422 xenografts, marked tumour regression is observed. Upon cessation of dosing, tumours in the 50 mg per kg once daily group shows tumour stasis whereas complete tumour eradication is observed in the 150 mg per kg once daily and 300 mg per kg twice per week groups. Tumour growth inhibition also correlates with statistically significant increased survival of mice bearing the more aggressive KARPAS-422 tumours, where spontaneous deaths occurres in vehicle-treated animals. No significant changes in any blood cell types at doses and times where efficacy is observed in tumour xenografts.
安全信息
"GSK126" 相关产品信息
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