1816331-66-4

中文名称:

1816331-66-4

中文同义词:

异柠檬酸脱氢酶1(IDH1)突变体抑制剂(GSK864)

英文名称:

GSK864

英文同义词:

GSK864;1H-Pyrazolo[4,3-c]pyridine-3,7-dicarboxamide, 1-[(4-fluorophenyl)methyl]-4,5,6,7-tetrahydro-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrol-2-ylcarbonyl)-, (7S)-;GSK864 >=98% (HPLC)

CAS号:

1816331-66-4

分子式:

C30H31FN6O4

分子量:

558.6

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1816331-66-4.mol

储存条件 

2-8°C

形态

powder

颜色

white to beige

旋光性 (optical activity)

[α]/D -66 to -76°, c = 0.5 in methanol

生物活性

GSK864是异柠檬酸脱氢酶1 (IDH1) 突变体抑制剂; 抑制IDH1突变体R132C，R132H和R132G的IC50值分别为8.8，15.2和16.6 nM。

靶点

IC50: 8.8 nM (IDH1 mutants R132C), 15.2 nM (IDH1 mutants R132H), 16.6 nM (IDH1 mutants R132G)

体外研究

GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells with an EC 50 of 320 nM by LCMS/MS analysis.

体内研究

Following intraperitoneal (IP) administration in CD-1 mice, significant concentrations of GSK864 are maintained in peripheral blood samples of mice for up to 24 hours. Analysis of BM cells for expression of markers of early differentiation reveals slightly increased numbers of huCD45 + CD38 + cells in R132C or R132H IDH1 mutant engrafted mice treated with GSK864.