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
* <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 is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
in vitro In liver cells, Deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Inhibition of PDEδ-KRAS interaction by Deltarasin suppresses proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS. [1]
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. [1]

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 small molecule (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 small molecules.
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.

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
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。

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