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Synonyms | Tyrphostin RG13022 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C16H14N2O2
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分子量 | 266.29 | CAS No. | 136831-48-6 | |
Solubility (25°C)* | 体外 | DMSO | 53 mg/mL (199.03 mM) | |
Ethanol | 5 mg/mL (18.77 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | RG 13022 (Tyrphostin RG13022) inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM. |
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in vitro | 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.[1]. |
in vivo | 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.[1]. |
細胞アッセイ | 細胞株 | HER14 Cells, MH-85 Cells |
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濃度 | 0-60 μM | |
反応時間 | 10 days | |
実験の流れ | 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. |
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動物実験 | 動物モデル | 4- to 6-week-old male BALB/c nu/nu mice |
投薬量 | 400 μg/mouse/day | |
投与方法 | IV |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。