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• 产品描述： RG 13022 (Tyrphostin RG13022)抑制免疫沉淀反应中EGF receptor的自磷酸化反应，IC50为4 µM

• 靶点： EGFR(Cell-free assay):4 μM;EGFR

• 体外研究：
  RG-13022 inhibits autophosphorylation of the EGF-receptor in HER 14 cells after an overnight incubation.The IC50 of RG-13022 is 5 μM. RG-13022 inhibits colony formation and DNA synthesis by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50 for RG-13022 is 1 μM for HER 14 colony formation and 3 μM for HER 14 DNA synthesis. RG-13022 also suppresses colony formation and DNA synthesis by EGF-stimulated MH-85 cells in a dose-dependent manner. The IC50 for RG-13022 on MH-85 cells is 7 μM for colony formation and 1.5 μM for DNA synthesis

• 体内研究：
  RG-13022 (400 μg/mouse/day) significantly inhibits MH-85 tumor growth. Because of slower tumor growth, MH-85 tumor-bearing animals receiving injections of RG-13022 show less cachexia and hypercalcemia, eat more food, and are more active than untreated MH-85 tumor-bearing animals. As a result of suppression of tumor growth, RG-13022 prolongs the life span of MH-85 tumor-bearing animals. Administration of mAb108 i.p. (1 mg/mouse/day) at 1, 5, and 10 days after MH-85 inoculation of RG-13022 (400 μg/mouse/day) for 14 days profoundly inhibits MH-85 growth in nude mice.

• 细胞实验： Cell lines: HER14 Cells, MH-85 Cells Concentrations: 0-60 μM Incubation Time: 10 days Method: MH-85 cells (100/well; 24-well plate) and HER 14 cells (200/dish; 10-cm dish) are plated in complete medium, either alpha MEM or DMEM, respectively, supplemented with 10% FCS. After overnight culture, the culture medium is switched to alpha MEM supplemented with 0.2% PCS and 50 ng/mL EGF (MH-85) or DMEM supplemented with 0.5% PCS and 50 ng/mL EGF (HER14). The cells are cultured in this medium in the presence or absence of increasing concentrations of RG-13022 for 10 days. At the end of culture, the cells are fixed with 4% (v/v) formaldehyde in calcium-magnesium-free phosphate-buffered saline for 15 min at room temperature and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope.

• 动物实验： Animal Models: 4- to 6-week-old male BALB/c nu/nu mice Dosages: 400 μg/mouse/day Administration: IV

• 参考文献：
  1. Yoneda T, et al. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 15;51(16):4430-5.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.755 ml	18.776 ml	37.552 ml
  5 mM	0.751 ml	3.755 ml	7.51 ml
  10 mM	0.376 ml	1.878 ml	3.755 ml
  50 mM	0.075 ml	0.376 ml	0.751 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 *