| 中文名称: | SGI-1027 | ||||
|---|---|---|---|---|---|
| 英文名称: | SGI-1027 | ||||
| 别名: | N-[4-[(2-氨基-6-甲基-4-嘧啶基)氨基]苯基]-4-(4-喹啉基氨基)苯甲酰胺;SGI-1027 抑制剂 N-(4-((2-amino-6-methylpyrimidin-4-yl)amino)phenyl)-4-(quinolin-4-ylamino)benzamide | ||||
| CAS No: | 1020149-73-8 | 分子式: | C27H23N7O | 分子量: | 461.52 |
| CAS No: | 1020149-73-8 | ||||
| 分子式: | C27H23N7O | ||||
| 分子量: | 461.52 | ||||
基本信息
|
产品编号：S10685 |
|||||
|
产品名称：SGI-1027 |
|||||
|
CAS: |
1020149-73-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
|
||||
|
分子式： |
溶于液体 |
-80℃ |
六个月 |
||
|
分子量 |
461.52 |
-20℃ |
一个月 |
||
|
化学名： |
|
||||
|
Solubility (25°C) |
体外 |
DMSO |
68mg/mL (147.33mM) |
||
|
Ethanol |
Insoluble |
||||
|
Water |
Insoluble |
||||
|
体内（现配现用） |
2% DMSO+30% PEG 300+2% Tween 80+ddH2O |
2mg/mL |
|||
|
＜1mg/ml表示微溶或不溶。 |
|||||
|
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
|||||
|
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
|||||
制备储备液
|
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
|
1mM |
2.1668mL |
10.8338mL |
21.6675mL |
|
5mM |
0.4334mL |
2.1668mL |
4.3335mL |
|
10mM |
0.2167mL |
1.0834mL |
2.1668mL |
|
50mM |
0.0433mL |
0.2167mL |
0.4334mL |
生物活性
|
产品描述 |
是 DNA 甲基转移酶 (DNMT) 抑制剂，对以 poly(dI-dC) 为底物的 DNMT3B，DNMT3A 和 DNMT1 的 IC50 值分别为 7.5μM，8μM 和 12.5μM。 |
||
|
靶点/IC50 |
DNMT1 |
DNMT3B |
DNMT3A |
|
6μM |
7.5μM |
8μM |
|
|
体外研究 |
SGI-1027 is a DNMT inhibitor, with IC50s of 7.5μM, 8μM, and 12.5μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate. SGI-1027 shows an IC50 of 6μM for DNMT1 (hemimethylated DNA). SGI-1027 (1, 2.5, or 5µM) causes selective degradation of DNMT1 in several human cancer cell lines, but shows little or no cytotoxic effect on rat hepatoma cells, and does not induce apoptosis in rat hepatoma cells[1]. SGI-1027 shows an EC50 of 0.9μM for hDNMT3A, and causes cytotoxicity on KG-1 cells, with an EC50 of 4.4μM. |
||
推荐实验方法(仅供参考)
|
激酶实验： |
|
To determine the nature of inhibition of DNMTase activity by SGI-1027, DNMT1 enzyme activity is measured in presence of a fixed concentration of SGI-1027 (0, 2.5, 5, and 10μM) while one of the two (Ado-Met or DNA) is varied in a particular reaction mixture. At a fixed concentration of DNA (500ng) varying concentrations of Ado-Met used are from 25-500nM,respectively.Similarly,final DNA concentrations are varied from (25-500ng) at 75nM Ado-Met. |
|
细胞实验: |
|
|
Rat hepatoma H4IIE cells are grown in DMEM supplemented with fetal bovine serum (10%) and calf serum (10%). Cells are seeded into 96-well plates and after 48h exposed to SGI-1027 at concentrations ranging from 0 to 300µM. The solubility is determined by Nephalometry techniques immediately after dosing and before harvesting the cells at 24h. Following the exposure period, the cells or their supernatant (culture medium) are analyzed for changes in cell proliferation (propidium iodide), membrane leakage (α-GST), mitochondrial function [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and cellular ATP], oxidative stress (intracellular GSH and 8-isoprostane), and apoptosis (caspase-3). The half-maximal toxic concentration (TC50) is determined from the dose-response curves. |
|
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
