中文名称: | NVP 231 | ||||
---|---|---|---|---|---|
英文名称: | NVP 231 | ||||
别名: | N-[2-(苯甲酰氨基)-6-苯并噻唑基]三环[3.3.1.13,7]癸烷-1-甲酰胺;NVP-231 抑制剂 N-[2-(Benzoylamino)-6-benzothiazolyl]-tricyclo[3.3.1.1(3,7)]decane-1-carboxamide | ||||
CAS No: | 362003-83-6 | 分子式: | C25H25N3O2S | 分子量: | 431.55 |
CAS No: | 362003-83-6 | ||||
分子式: | C25H25N3O2S | ||||
分子量: | 431.55 |
基本信息
产品编号:N10625 |
|||||
产品名称:NVP 231 |
|||||
CAS: |
362003-83-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
||||
分子式: |
溶于液体 |
-80℃ |
六个月 |
||
分子量 |
431.55 |
-20℃ |
一个月 |
||
化学名: |
|
||||
Solubility (25°C) |
体外 |
DMSO |
86mg/mL (199.28mM) |
||
Ethanol |
8mg/mL (18.53mM) |
||||
Water |
Insoluble |
||||
体内(现配现用) |
|
|
|||
<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 |
2.3172mL |
11.5861mL |
23.1723mL |
5mM |
0.4634mL |
2.3172mL |
4.6345mL |
10mM |
0.2317mL |
1.1586mL |
2.3172mL |
50mM |
0.0463mL |
0.2317mL |
0.4634mL |
生物活性
产品描述 |
一种强效、特异、可逆的神经酰胺激酶 (CerK) 抑制剂 (IC50=12nM),可竞争性地抑制神经酰胺与 CerK 的结合。 |
|
靶点/IC50 |
12nM (CerK); apoptosis |
|
体外研究 |
NVP-231 (0-500 nM; 24 hours) gradually reduces the cellular CerK activity, as measured by NBD-C1P formation,demonstrating that NVP-231 active in transfected cells. The IC50 for CerK in this cellular system is 59.70 ± 12nM.NVP-231 (0-1000nM; 48 hours) decreases cell viability as a dose-dependent manner. This compound shows IC50 values of 1μM in MCF-7 cells and 500nM in NCI-H358 cells.NVP-231 (1μM; 24-72 hours) induces caspase-3 and caspase-9 cleavage in both cell lines. However, the highest caspase-3 and caspase-9 cleavage and activation occurred at 24 hours in MCF-7 cells, then decreases again. In NCI-H358 cells, caspase3 and caspase-9 cleavage occurrs continuously over 72 hours.NVP-231 (0-500nM; 24 hours) causes a concentration-dependent up-regulation of cyclin B1 phosphorylation at Ser133 and a reduction of CDK1 phosphorylation at Tyr15. The total CDK1 expression also declined upon CerK inhibition. Cell Viability Assay |
|
Cell Line: |
MCF-7 cells; NCI-H358 cells |
|
Concentration: |
0nM, 10nM, 100nM, 300nM, 500nM, 1000nM |
|
Incubation Time: |
48 hours |
|
Result: |
Reduced MCF-7 cells and NCI-H358 cells in a concentration manner. |
|
Apoptosis Analysis |
||
Cell Line: |
MCF-7 cells; NCI-H358 cells |
|
Concentration: |
1000nM |
|
Incubation Time: |
24-72 hours |
|
Result: |
Increases caspase-3 and caspase-9 cleavage in MCF-7 and NCI-H358 cells. |
|
Western Blot Analysis |
||
Cell Line: |
MCF-7 cells; NCI-H358 cells |
|
Concentration: |
Concentration: 0nM, 100nM, 300nM, 500nM |
|
Incubation Time: |
24 hours |
|
Result: |
Decreased p-cyclin B1, p-CDK1 as a concentration manner. |
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 )