中文名称: | GSK2801 | ||||
---|---|---|---|---|---|
英文名称: | GSK2801 | ||||
别名: | Epigenetic Reader Domain GSK-2801;1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone | ||||
CAS No: | 1619994-68-1 | 分子式: | C20H21NO4S | 分子量: | 371.45 |
CAS No: | 1619994-68-1 | ||||
分子式: | C20H21NO4S | ||||
分子量: | 371.45 |
基本信息
产品编号:G10241 |
|||||
产品名称:GSK2801 |
|||||
CAS: |
1619994-68-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
||||
分子式: |
溶于液体 |
-80℃ |
六个月 |
||
分子量: |
371.45 |
-20℃ |
一个月 |
||
化学名: |
|
||||
Solubility (25°C) |
体外 |
DMSO |
74mg/mL warmed with 50ºC water bath (199.21mM) |
||
Ethanol |
7mg/mL warmed with 50ºC water bath (18.84mM) |
||||
Water |
Insoluble |
||||
体内(现配现用) |
0.5% CMC+1% Tween 80 |
30mg/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 |
2.6922mL |
13.4608mL |
26.9215mL |
5mM |
0.5384mL |
2.6922mL |
5.3843mL |
10mM |
0.2692mL |
1.3461mL |
2.6922mL |
50mM |
0.0538mL |
0.2692mL |
0.5384mL |
生物活性
产品描述 |
一种用于BAZ2B/a溴化物的选择性化学探针。 |
|
靶点/IC50 |
BAZ2B |
BAZ2A |
136nM(Kd) |
257nM(Kd) |
|
体外研究 |
GSK2801 binds TAF1L with an affinity KB of 0.31μM (KD:3.2μM) and a binding enthalpy change ΔH of−8.6 kcal/mol.ITC experiments using the bromodomain of BRD9 results in the determination of an affinity KB of 0.826μM (KD:1.1μM) and ΔH of−9.8 kcal/mol.GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes.In 2D cultures,enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence.In spheroid cultures,combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells.Thus,GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC. |
|
体内研究 |
In order to determine the suitability of GSK2801 for in vivo experiments,pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured.GSK2801 has reasonable in vivo exposure after oral dosing,modest clearance, and reasonable plasma stability. |
推荐实验方法(仅供参考)
动物实验: |
|
动物模型 |
雄性 CD1 小鼠 |
剂量 |
30mg/kg |
给药处理 |
i.p.,p.o. |
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 )