RBC8

製品コードS7606 バッチS760601

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C25H20N4O3

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.

溶剤液(一定の濃度)を調合する

生物活性

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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human lung cancer cell lines H2122, H358, H460 and Calu-6
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.

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2016, 7(15): 20561-20573]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

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。

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