• 产品描述： Lomeguatrib is a O6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ∼6 nM in MCF-7 cells.

• 靶点： MGMTcc:6 nM (IC50, in MCF-7 cells);MGMT:9 nM (IC50);DNAMethyltransferase; DNAAlkylation

• 体外研究：
  Lomeguatrib (Compound 10) is a O6-methylguanine methyltransferase (MGMT) inhibitor, with an IC50 of 9 nM in cell-free assay and ∼6 nM in MCF-7 cells. Lomeguatrib (10 μM) substantially increases the growth inhibitory effects of temozolomide in MCF-7 cells (D60=10 μM with Lomeguatrib vs 400 μM without)

• 体内研究：
  Lomeguatrib (20 mg/kg i.p.) completely inactivates MGMT within 2 h, but shows no significant effect on tumor growth in MCF-7 xenografts

• 参考文献：
  1. Reinhard J, et al. Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J Med Chem. 2001 Nov 22;44(24):4050-61. 2. Clemons M, et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. Br J Cancer. 2005 Nov 14;93(10):1152-6.

• 溶解性： soluble  in  DMSO

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.066 ml	15.329 ml	30.659 ml
  5 mM	0.613 ml	3.066 ml	6.132 ml
  10 mM	0.307 ml	1.533 ml	3.066 ml
  50 mM	0.061 ml	0.307 ml	0.613 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 *