Kobe0065

製品コードS8303 バッチS830301

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

C15H11ClF3N5O4S
分子量 449.79 CAS No. 436133-68-5
Solubility (25°C)* 体外 DMSO 89 mg/mL (197.87 mM)
Ethanol 13 mg/mL (28.9 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Kobe0065 is an H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
in vitro Kobe0065-family compounds bind to Ras⋅GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras⋅GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition[1].
in vivo Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 NIH 3T3 cells
濃度 2 and 20 μM
反応時間 1 h
実験の流れ NIH 3T3 cells are transfected with pEF-BOS-HA-H-Ras(G12V) or an empty vector and treated with the 2 and 20 μM compound or the vehicle (DMSO) in the presence of 2% FBS for 1 h. Cell lysate is subjected to detection of c-Raf-1 coimmunoprecipitated with an anti-H-Ras antibody and total c-Raf-1 by Western blotting with an anti-c-Raf-1 antibody. Immunoprecipitated H-Ras(G12V) are detected by an anti-HA antibody.
動物実験 動物モデル A xenograft of SW480 cells in nude mice.
投薬量 80 mg/kg and 160 mg/kg
投与方法 oral administration

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：

Glycyrrhetinic acid binds to the conserved P-loop region and interferes with the interaction of RAS-effector proteins. [ Acta Pharm Sin B, 2019, 9(2):294-303] PubMed: 30976491
RAF kinases are stabilized and required for dendritic cell differentiation and function. [ Cell Death Differ, 2019, 10.1038/s41418-019-0416-4] PubMed: 31541179

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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