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• 产品描述： 3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine derivative with antitumor activity.

• 靶点： IC50: 21 nM (breast MDA-MB-231), 19 nM (pancreas PANC-1), 17 nM (colon HCT 116), 19 nM (prostate PC3), 14 nM (ovary OVCAR-3), 32 nM (melanoma SK-MEL-28), 22 nM (kidney Caki-1), 32 nM (glioblastoma SNB19);Others

• 体外研究：
  3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine derivative, extracted from the reference, compound 7b.3-arylisoquinolinamine derivative (7b) shows more effective activity against Paclitaxel-resistant HCT-15 human colorectal cancer cell lines when compared to the original cytotoxic cancer drug, Paclitaxel. The cell cycle dynamics is analyzed by flow cytometry. Treatment of human HCT-15 cells with 3-arylisoquinolinamine derivative (7b) blocks or delays the progression of cells from G0/G1 phase into S phase, and induces cell death. Treatment with 3-arylisoquinolinamine derivative (7b) also significantly inhibits the growth of tumors and enhances tumor regression in a Paclitaxel-resistant HCT-15 xenograft model. 3-arylisoquinolinamine derivative (7b) inhibits the cell growth at IC50 value ranges from 14 nM to 32 nM in the human cancer cells tested. In cell cycle analysis using HCT-15 cells, treatment of 1 nM of 3-arylisoquinolinamine derivative (7b) displays a significant increase in G0/G1 phase at 24 h with a decrease in G2/M phase, but the increase of G0/G1 phase at 48 h is not significant. At higher concentration of 3-arylisoquinolinamine derivative (7b) (10 nM), there are a significant increase in G0/G1 phase and decrease in G2/M phase, and an emergence of sub-G1phase, at both 24 h and 48 h. 3-arylisoquinolinamine derivative (7b) blocks or delays the progression of cells from G0/G1 phase into S phase, and induces cell death. 3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine

• 体内研究：
  3-arylisoquinolinamine derivative (Compound 13) has higher antitumor efficacy (69.2 % inhibition) than that of the control drug, Paclitaxel (48.8 % inhibition) in the inhibition of growth of tumor in an animal model

• 参考文献：
  1. Yang SH, et al. Synthesis, in vitro and in vivo evaluation of 3-arylisoquinolinamines as potent antitumor agents. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5277-81. 2. Young Bok Lee, et al. 5, 6, or 7-substituted-s- (hetero)arylisoquinolinamine derivatives as antitumor agents. WO 2008063548 A2.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.409 ml	17.044 ml	34.087 ml
  5 mM	0.682 ml	3.409 ml	6.817 ml
  10 mM	0.341 ml	1.704 ml	3.409 ml
  50 mM	0.068 ml	0.341 ml	0.682 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 *