• 产品描述： BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity

• 靶点： CDK8:1.1 nM (IC50);CDK

• 体外研究：
  BI-1347 (150 nM; 44 h) enhances granzyme B (GZMB+) production in mouse splenic NK cells. BI-1347 (0.1 nM-10 μM; 24 h) treatment increases perforin secretion from NK92MI cells. Western Blot Analysis Cell Line: Mouse splenic NK cells Concentration: 150 nM Incubation Time: 44 hours Result: Increased the proportion of granzyme B-positive NK cells by approximately 4-fold. Western Blot Analysis Cell Line: Human NK92MI cells Concentration: 0.1 nM-10 μM Incubation Time: 24 hours Result: Increased perforin levels with an EC50 value of 7.2 nM.

• 体内研究：
  BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1S727 phosphorylation and shows anti-tumor activity in vivo. BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model. Animal Model: B16-F10-luc2 syngeneic melanoma model Dosage: 10 mg/kg Administration: Oral gavage; 10 mg/kg; once daily; 30 d Result: Reduced phosphorylation of STAT1S727 for at least 6 h by 60%.Showed minimal effect on body weight at 10 mg/kg.Showed lower tumor burden both on day 23 and 29, compared to the control group.

• 参考文献：
  1. Harald Engelhardt, et al. New phenylpyrazolylacetamide compounds and derivatives as cdk8/cdk19 inhibitors. 2. Hofmann MH, et al. Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance. Mol Cancer Ther. 2020 Apr;19(4):1018-1030.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.806 ml	14.028 ml	28.057 ml
  5 mM	0.561 ml	2.806 ml	5.611 ml
  10 mM	0.281 ml	1.403 ml	2.806 ml
  50 mM	0.056 ml	0.281 ml	0.561 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。

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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 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *