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• 产品描述： BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family

• 靶点： BRD9:75 nM (IC50);BRD9:14 nM (Kd);BRD7:3.4 μM (IC50);BRD7:239 nM (Kd);EpigeneticReaderDomain

• 体外研究：
  BI-9564 (<5 μM) shows no activity against 324 kinases, and at 10 μM, an inhibition >40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC50 of 800 nM. BI-9564 shows Kd of 73 nM for BRD7, and is >10-fold more selective for BRD9 over the highly homologues bromodomain BRD7, which has been implied as a tumor suppressor and is down-regulated in cancer cells

• 体内研究：
  BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles for in vivo proof-of-concept studies. BI-9564 results in a modest but significant additional survival benefit of 2 days compared to survival of the control group in a xenograft model of human AML

• 参考文献：
  1. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75. 2. Rezaul M. Karim, et al. An Advanced Tool To Interrogate BRD9. J. Med. Chem., 2016, 59 (10), pp 4459-4461

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.83 ml	14.148 ml	28.295 ml
  5 mM	0.566 ml	2.83 ml	5.659 ml
  10 mM	0.283 ml	1.415 ml	2.83 ml
  50 mM	0.057 ml	0.283 ml	0.566 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 *