Deltarasin

製品コードS7224 バッチS722401

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

C40H37N5O
分子量 603.75 CAS No. 1440898-61-2
Solubility (25°C)* 体外 DMSO 100 mg/mL (165.63 mM)
Ethanol 100 mg/mL (165.63 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5mg/ml (8.28mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5mg/ml (8.28mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
* <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 Deltarasin は、精製された PDEδ への結合 Kd が 38 nM である KRAS-PDEδ 相互作用の低分子阻害剤です。
in vitro In liver cells, Deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Inhibition of PDEδ-KRAS interaction by this compound suppresses proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS.
in vivo Deltarasin (10 mg/kg i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumour cell xenografts.

プロトコル(参考用のみ)

キナーゼアッセイ KD measurements
KD values are measured by fluorescence polarization measurements. For direct titrations, increasing amounts of PDEδ are added to a solution containing 50-100 nM labelled small molecule in 200 µl PBS buffer. For displacement titrations, increasing amounts of the small molecules in DMSO are directly added to fluorescein-labelled atorvastatin (24 nM) and His6-tagged PDEδ (40 nM) in 200 µl PBS-buffer (containing 0.05% CHAPS, 1% DMSO), keeping the concentration of fluorescein-labelled atorvastatin, PDEδ and DMSO constant. For KD measurements using isothermal titration calorimetry, PDEδ protein (280 µM) is titrated to this compound (30 µM) in Tris/HCl buffer (temperature 25 °C). In the Tm shift assays, protein melting points are detected by circular dichroism spectroscopy in the presence of this chemical.
動物実験 動物モデル Mice bearing Panc-Tu-I xenografts
投薬量 10 mg/kg bid
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/23698361/

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：

Detection of Ras nanoclustering-dependent homo-FRET using fluorescence anisotropy measurements [ Eur J Cell Biol, 2023, 102(2):151314] PubMed: 37058825
Comprehensive Analysis of the Expression and Clinical Significance of RAS Family Members in Non-Small Cell Lung Cancer Based on Bioinformatics Data [ Appl. Sci, 2023, 13(1), 166] PubMed: None
MEK nuclear localization promotes YAP stability via sequestering β-TrCP in KRAS mutant cancer cells. [ Cell Death Differ, 2019, 26(11):2400-2415] PubMed: 30833665
EPHA2 feedback activation limits the response to PDEδ inhibition in KRAS-dependent cancer cells. [ Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y] PubMed: 31316177
Myeloid-derived interleukin-1β drives oncogenic KRAS-NF-κΒ addiction in malignant pleural effusion. [ Nat Commun, 2018, 9(1):672] PubMed: 29445180
Myeloid-derived interleukin-1β drives oncogenicKRAS-NF-κΒ addiction in malignant pleural effusion [ Nature Communications, 2018, 672-2018)] PubMed: None
Inhibition of KRAS-dependent lung cancer cell growth by deltarasin: blockage of autophagy increases its cytotoxicity [ Cell Death Dis, 2018, 9(2):216] PubMed: 29440631

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。