| 产品描述： | BAY1251152 是一种有效的 PTEFb/CDK9 的抑制剂，在酶法测定中对CDK9的IC50值为3 nM，相对于其他CDK的选择性至少为50倍。BAY1251152 结合并阻断CDK9的磷酸化和激酶活性，从而防止PTEFb介导的RNA Pol II活化，并导致各种抗凋亡蛋白的基因转录受到抑制 |
| 靶点： |
CDK9(Cell-free assay):3 nM |
| 体外研究： |
BAY 1251152 (compound 2) significantly inhibits CDK9 and CDK2 with IC50 of 3 nM and 360 nM, respectively. BAY 1251152 (compound 2) shows cellular potency in MOLM13 with IC50 of 29 nM |
| 体内研究： |
BAY 1251152 demonstrates excellent efficacy upon i.v. treatment in xenograft models (e.g. MOLM13) in mice and rats. BAY 1251152 is currently being evaluated in Phase I studies to determine the safety, tolerability, pharmacokinetics and initial pharmacodynamic biomarker response in patients with advanced cancer |
| 细胞实验： |
Cell lines: HeLa, NCI-H460, A2780, DU 145, HeLa-MaTu-ADR, Caco-2, B16F10, MOLM-13 Concentrations: 0.001 μM - 10 μM Incubation Time: 4 days Method: Cultivated tumour cells are plated in a 96-well multititer plate in 200 of their 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 is 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 0.001 -10 μM; the final concentration of the solvent dimethyl sulfoxide is 0.5%). The cells are incubated for 4 days in the presence of test substances. |
| 动物实验： |
Animal Models: mice and rats with xenograft models (eg. MOLM13) Dosages: -- Administration: IV |
| 参考文献： |
1. Ulrich LÜCKING, et al. 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group. WO2014076091Al. 2. Ulrich T. Luecking, et al. Abstract 984: Identification of potent and highly selective PTEFb inhibitor BAY 1251152 for the treatment of cancer: from p.o. to i.v. application via scaffold hops. Cancer Res 2017;77(13 Suppl):Abstract nr 984. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.473 ml |
12.363 ml |
24.726 ml |
| 5 mM |
0.495 ml |
2.473 ml |
4.945 ml |
| 10 mM |
0.247 ml |
1.236 ml |
2.473 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.495 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