|2-(4-(4-(异喹啉-4-基)苯基)-1H-吡唑-1-基)-N,N-二甲基乙酰胺|CsnPharm

CAS No.: 2163056-91-3

BI-1347 Catalog No. CSN25300

Synonyms: BI-1347

BI-1347 is a potent CDK8 inhibitor with an IC50 of 1.1 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Members of the cyclin-dependent kinase family coordinate regulatory events during the cell cycle as well as transcription. Cyclin-dependent kinase 8 (CDK8) and CDK19 regulate transcription via interaction with the mediator complex and by phosphorylation of transcription factors. BI-1347 is a highly selective and potent inhibitor of CDK8/19 that potently decreases the phosphorylation of STAT1^S727. BI-1347 showed high potency with IC₅₀ value in the CDK8 kinase assay of 1.4 nM. In C57BL/6 mice, a significant reduction in STAT1^S727 phosphorylation was observed in splenocytes upon treatment with 3 mg/kg of BI-1347. In B16-F10-luc2 tumor bearing mice, a daily oral dose of 10 mg/kg BI-1347 resulted in TGI (tumor growth inhibition) of 94% on day 23 and 88% on day 29 and a median survival advantage of 4 days compared with vehicle-treated animals. In vivo imaging revealed lower tumor burden in the BI-1347–treated group both on days 23 and 29, compared with the control group^[1].
参考文献

[1] Hofmann MH, Mani R, Engelhardt H, et al. Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance. Mol Cancer Ther. 2020;19(4):1018-1030

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8057 mL
- 14.0284 mL
- 28.0568 mL
- 5 mM
- 0.5611 mL
- 2.8057 mL
- 5.6114 mL
- 10 mM
- 0.2806 mL
- 1.4028 mL
- 2.8057 mL

技术信息

CAS号

2163056-91-3

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H20N4O

运输

蓝冰

分子量

356.42

别名

BI-1347

溶解度

DMSO	71.0 mg/mL (199.2 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (8.4 mM)

动物实验配方

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