| 产品描述： | Empesertib (BAY1161909, Mps1-IN-5) 是一种三唑并吡啶的衍生物，是 serine/threonine monopolar spindle 1 (Mps1) kinase 的口服生物利用型选择性抑制剂，IC50值 <1 nM。 Empesertib 具有潜在的抗肿瘤活性 |
| 靶点： |
Mps1(Cell-free assay):1 nM;Kinesin |
| 体外研究： |
Empesertib (BAY1161909) is a very effective Mps-1 inhibitor with an IC50 lower than or equal to 1 nM (more potent than 1 nM) in an Mps-1 kinase assay with a concentration of 1 μM/2 mM ATP, and an IC50 lower than 400 nM in a HeLa cell proliferation assay |
| 体内研究： |
Empesertib (BAY1161909) is a very effective Mps-1 inhibitor with a maximum oral bioavailability (Fmax) in rat that is higher than 70%, determined by means of rat liver microsomes, and a maximum oral bioavailability (Fmax) in dog that is higher than 50%, determined by means of dog liver microsomes, and a maximum oral bioavailability (Fmax) in human that is higher than 60%, determined by means of human liver microsomes |
| 细胞实验： |
Cell lines: Cultivated tumor cells Concentrations: 0.01 μM-30 μM Incubation Time: 4 days Method: Cultivated tumor cells are plated at a density of 5000 cells/well (MCF7, DU145, HeLa-MaTu-ADR), 3000 cells/well (NCI-H460, HeLa-MaTu, HeLa), or 1000 cells/well (B16F10) in a 96-well multititer plate in 200 μl of their 5 respective growth medium supplemented 10% fetal calf serum. After 24 hours, the cells of one plate (zero-point plate) are stained with crystal violet, while the medium of the other plates was replaced by fresh culture medium (200 μl), to which the test substances are added in various concentrations (0 μM, as well as in the range of 0.01-30 μM; The cells are incubated for 4 days in the presence of test substances. Cell proliferation is determined by staining the cells with crystal violet: the cells are fixed by adding 20 μl/measuring point of an 11 % glutaric aldehyde solution for 15 minutes at room temperature. After three washing cycles of the fixed cells 15 with water, the plates are dried at |
| 动物实验： |
Animal Models: rat, dog and humans Dosages: 1-2 mg/mL Administration: Oral gavage, IV |
| 参考文献： |
1. Volker Schulze, et al. WO2014198647A2. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.787 ml |
8.935 ml |
17.87 ml |
| 5 mM |
0.357 ml |
1.787 ml |
3.574 ml |
| 10 mM |
0.179 ml |
0.893 ml |
1.787 ml |
| 50 mM |
0.036 ml |
0.179 ml |
0.357 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京