價(jià)格 | ¥373 | ¥738 | ¥1170 |
包裝 | 2mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-12 |
中文名稱:化合物 Deltarasin | 英文名稱:Deltarasin |
CAS:1440898-61-2 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.06% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): T6462 |
名稱 | Deltarasin |
描述 | Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
激酶實(shí)驗(yàn) | 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. |
體外活性 | 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] |
體內(nèi)活性 | Deltarasin (10 mg/kg i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumor cell xenografts [1]. The finding may inspire novel drug discovery efforts aimed at the development of drugs targeting oncogenic RAS. |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 93 mg/mL (154 mM) DMSO : 93 mg/mL (154 mM) |
關(guān)鍵字 | Phosphodiesterase (PDE) | inhibit | Deltarasin | Inhibitor | Ras |
相關(guān)產(chǎn)品 | Icariin | Vardenafil hydrochloride | Apremilast | Indomethacin | Roflumilast | Sildenafil citrate | Theophylline | Acefylline | Theobromine | Theophylline monohydrate | Isoprenaline hydrochloride | Doxofylline |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 抗結(jié)直腸癌化合物庫 | 激酶抑制劑庫 | 抗肝癌化合物庫 | GPCR靶點(diǎn)分子庫 | 膜蛋白靶向化合物庫 | 疼痛相關(guān)化合物庫 | PPI抑制劑庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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