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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H13F3N4O |
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分子量 | 334.1 | CAS No. | 1637739-82-2 | |
Solubility (25°C)* | 体外 | DMSO | 66 mg/mL warmed with 50ºC water bath (197.54 mM) | |
Ethanol | 20 mg/mL warmed with 50ºC water bath (59.86 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 | BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA. |
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in vitro | In both the H2122 and H358 cell lines, BQU57 inhibits both RalA and RalB activation, and thus causes cell growth inhibition. [1] |
in vivo | In mice bearing human lung H2122 tumors, BQU57 (50 mg/kg, i.p.) significantly inhibits activation of both RalA and RalB, and causes dose-dependent tumor growth inhibition. [1] |
細胞アッセイ | 細胞株 | Human lung cancer lines, H2122, H358, H460 and Calu6 |
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濃度 | ~10 μM | |
反応時間 | 48 hours | |
実験の流れ | Growth inhibition on human lung cancer cells by the compounds are measured under anchorage-independent conditions in soft agar. Cells are seeded into 6-well plates (coated with a base layer made of 2.0 mL of 1% low-melting-point agarose) at 15,000 cells per well in 3.0 mL of 0.4% low-melting-point agarose containing various concentration of drug. Two to four weeks (depending on cell line) after incubation, cells are stained with 1.0 mg/mL Nitro Blue Tetrazolium and colonies are counted under a microscope. The IC50 values are defined as the concentration of drug that resulted in 50% reduction in colony number compared to DMSO treated control. After 48 hr, cells are subjected to the soft agar colony formation assay. | |
動物実験 | 動物モデル | Mice bearing human lung H2122 tumors |
投薬量 | 50 mg/kg | |
投与方法 | i.p. |
RalA and RalB relocalization to depolarized mitochondria depends on clathrin-mediated endocytosis and facilitates TBK1 activation. [ PLoS One, 2019, 14(4):e0214764] | PubMed: 30995277 |
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。