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GSK126
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK126图片
CAS NO:1346574-57-9
包装:2mg, 5mg, 10mg, 50mg

EZH2 inhibitor
GSK2816126A

生物活性

GSK126是一种高活性,S-腺苷-蛋氨酸竞争性EZH2甲基转移酶抑制剂,Ki为0.5 nM。GSK126 decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice.


化学数据

分子量526.67
分子式C31H38N6O2
CAS号1346574-57-9
纯度98.49%
溶解性(25°C)DMSO 10 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系EZH2 wildtype or mutant B-cell lymphoma cell lines
方法Cell proliferation assay. The optimal cell seeding was determined empirically for all cell lines by examining the growth of a wide range of seeding densities in a 384-well format to identify conditions that permitted proliferation for 6 days. Cells were then plated at the optimal seeding density 24 h before treatment (in duplicate) with a 20-point twofold dilution series of GSK126 or 0.15% DMSO. Plates were incubated for 6 days at 37℃ in 5% CO2. Cells were then lysed with CellTiter-Glo (CTG) (Promega) and chemiluminescent signal was detected with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells was harvested at the time of compound addition (T0) to quantify the starting number of cells. CTG values obtained after the 6 day treatment were expressed as a percent of the T0 value and plotted against compound concentration. Data were fit with a four-parameter equation to generate a concentration response curve and the concentration of GSK126 required to inhibit 50% of growth (growth IC50) was determined.
浓度0~100μM
处理时间6 days

动物实验
动物模型Pfeiffer or KARPAS-422 cells tumour xenograft in mice
配制20% captisol adjusted to pH 4–4.5 with 1 N acetic acid.
剂量0.2 ml per 20 g body weight
给药处理intraperitoneally

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM1.8987 mL9.4936 mL18.9872 mL
5 mM0.3797 mL1.8987 mL3.7974 mL
10 mM0.1899 mL0.9494 mL1.8987 mL
 
 
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