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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 | C25H20N4O3 |
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分子量 | 424.45 | CAS No. | 361185-42-4 | |
Solubility (25°C)* | 体外 | DMSO | 84 mg/mL (197.9 mM) | |
Water | Insoluble | |||
Ethanol | 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 | RBC8 is a selective inhibitor of the GTPases RalA and RalB by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases Ras and RhoA. |
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in vitro | In living cells, RBC8 also reduces the activation of RalA by inducing chemical shift changes in RalB–GDP. In Ral-dependent lines H2122 and H358, RBC8 causes anchorage-independent growth inhibition with IC50 of 3.5 µM and 3.4 µM, respectively. [1] |
in vivo | In mice bearing H358 xenografts, RBC8 (50 mg/kg i.p.) inhibits tumor growth via specific inhibition of RalA and RalB. [1] |
細胞アッセイ | 細胞株 | Human lung cancer cell lines H2122, H358, H460 and Calu-6 |
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濃度 | ~10 μM | |
反応時間 | 2-4 weeks | |
実験の流れ | Growth inhibition of human lung cancer cells by the compounds is 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 the cell line) after incubation, the cells are stained with 1.0 mg ml−1 nitroblue tetrazolium, and colonies are counted under a microscope. The IC50 values are defined as the concentration of drug that resulted in a 50% reduction in colony number compared with the DMSO-treated control. | |
動物実験 | 動物モデル | Mice bearing H358 xenografts |
投薬量 | 50 mg/kg | |
投与方法 | i.p. |
Data from [Data independently produced by , , Oncotarget, 2016, 7(15): 20561-20573]
FOXD1-dependent RalA-ANXA2-Src complex promotes CTC formation in breast cancer [ J Exp Clin Cancer Res, 2022, 41(1):301] | PubMed: 36229838 |
RAL GTPases mediate multiple myeloma cell survival and are activated independently of oncogenic RAS. [ Haematologica, 2019, 10.3324/haematol.2019.223024] | PubMed: 31601693 |
RalA, a GTPase targeted by miR-181a, promotes transformation and progression by activating the Ras-related signaling pathway in chronic myelogenous leukemia. [ Oncotarget, 2016, 7(15):20561-73] | PubMed: 26967392 |
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。