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• 產品描述： GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).

• 靶點： IC50: 22 nM (BRD4), 31 nM (BRD3), 41 nM (BRD2);Apoptosis;?EpigeneticReaderDomain

• 體外研究：
  A panel of neuroblastoma cell lines are treated with GSK1324726A (I-BET726), and observed potent growth inhibition and cytotoxicity in most cell lines irrespective of MYCN copy number or expression level. All neuroblastoma cell lines tested exhibit potent growth inhibition, with a median growth IC50 value (gIC50; inhibitor concentration resulting in 50% growth inhibition) equal to 75 nM。

• 體內研究：
  GSK1324726A (I-BET726) inhibits neuroblastoma tumor growth. In the SK-N-AS model, mice in the vehicle group are euthanized on day 14 due to large tumor size. While there is no significant difference in tumor growth between the vehicle and GSK1324726A (5 mg/kg) group, 58% tumor growth inhibition (TGI) is observed in the GSK1324726A (15 mg/kg) group on day 14 of the study (n=9; p=0.006). Mice in the GSK1324726A (15 mg/kg) group are treated for an additional 7 days before tumor volume reaches a level comparable to that observed in the vehicle group, at which point the study is terminated. Tumors in the CHP-212 model grow much more slowly. After 42 days, tumors in vehicle-treated mice are only half the size those in the SK-N-AS model at the end of the study (Day 14). In the CHP-212 model, treatment with 5 mg/kg GSK1324726A results in TGI equal to 50% (n=8; p=0.1816), and mice in the 15 mg/kg group exhibits a TGI of 82% at the end of the study (n=5; p=0.0488)。

• 參考文獻：
  1. Wyce A, et al. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8(8):e72967. 2. Gosmini R, et al. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31.

• 溶解性： soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.299 ml	11.497 ml	22.993 ml
  5 mM	0.46 ml	2.299 ml	4.599 ml
  10 mM	0.23 ml	1.15 ml	2.299 ml
  50 mM	0.046 ml	0.23 ml	0.46 ml

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本計算器可幫助您計算出特定溶液中溶質的質量、溶液濃度和體積之間的關系，公式為：

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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