• 产品描述： BI 894999 是一种有效的、选择性的 BET 抑制剂，可抑制BRD4-BD1和BRD4-BD2与乙酰化组蛋白的结合，对应的IC50值分别为5 nM和41 nM。BI 894999 对BRD2/3/4和BRDT (Kd为0.49-1.6 nM) 具有高度选择性，相对于BRD4-BD1具有至少200倍的选择性

• 靶点： BET; BRD4-BD1(Cell-free assay):5 nM; BRD4-BD2(Cell-free assay):41 nM;EpigeneticReaderDomain

• 体外研究：
  BI 894999 is highly active in AML cell lines, primary patient samples. BI 894999 targets super-enhancer-regulated oncogenes and other lineage-specific factors, which are involved in the maintenance of the disease state

• 体内研究：
  BI 894999 is active as monotherapy in AML xenografts, and in addition leads to strongly enhanced antitumor effects in combination with CDK9 inhibitors

• 细胞实验： Cell lines: MV-4-11B, THP-1, MOLM-13
  Concentrations: 10 nM, 100 nM, various concentrations
  Incubation Time: 4h, 24h, 79 h, 96 h
  Method:
  For viability assay, the cells are plated in 96-well flat-bottom microtiter plates and incubated overnight at 37°C in a CO2 incubator. BI 894999 is added at various concentrations for 72 hours or 96 hours. After 6-hour incubation with Alamar Blue solution at 37°C, fluorescence is measured using an excitation wavelength of 531 nm and emission at 595 nm.

• 动物实验： Animal Models: 6-8 week old female NMRI-nude/CIEA-NOG miceDosages: 1 mg/kg, 2 mg/kg, 4 mg/kg, 12 mg/kgAdministration: Oral gavage

• 参考文献：
  1. Daniel Gerlach, et al. The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML. Oncogene. 2018 May;37(20):2687-2701. 2. Ulrike Tontsch-Grunt, et al. Synergistic activity of BET inhibitor BI 894999 with PLK inhibitor volasertib in AML in vitro and in vivo. Cancer Lett. 2018 May 1;421:112-120.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.328 ml	11.641 ml	23.282 ml
  5 mM	0.466 ml	2.328 ml	4.656 ml
  10 mM	0.233 ml	1.164 ml	2.328 ml
  50 mM	0.047 ml	0.233 ml	0.466 ml

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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 *