S83009 |
RG13022 |
| 源叶(MedMol) | 98% |
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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
- 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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