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• 产品描述： CGI-1746 is a potent and highly selective inhibitor of the Btk with IC50 of 1.9 nM.

• 靶点： IC50: 1.9 nM (Btk);BTK; Autophagy

• 体内研究：
  CGI1746 abrogates B cell-dependent arthritis. CGI1746 treatment (100 mg/kg, s.c, twice-daily dosing) results in significant inhibition (97%) of overall clinical arthritis scores. CGI1746 treatment substantially reduces TNFα, IL-1β and IL-6, as well as MCP1 and MIP-1α on both the mRNA and protein level in the passive anti-collagen II antibody-induced arthritis (CAIA) model. CGI1746 shows comparable efficacy to TNFα blockade and significantly reduces clinical scores, as well as joint inflammation, in mice or rats with established arthritis

• 参考文献：
  1. Di Paolo, Julie A. et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nature Chemical Biology (2011), 7(1), 41-50 2. Kokabee L, et al. Bruton's tyrosine kinase is a potential therapeutic target in prostate cancer. Cancer Biol Ther. 2015;16(11):1604-15

• 溶解性： DMSO  :  ≥  50  mg/mL  (86.25  mM)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.725 ml	8.625 ml	17.25 ml
  5 mM	0.345 ml	1.725 ml	3.45 ml
  10 mM	0.173 ml	0.863 ml	1.725 ml
  50 mM	0.035 ml	0.173 ml	0.345 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 *