化合物Deltarasin T6462
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
2 mg | 1440898-61-2 | ¥373.00 | 询底价 |
1 mL | 1440898-61-2 | ¥995.00 | 询底价 |
10 mg | 1440898-61-2 | ¥1,170.00 | 询底价 |
25 mg | 1440898-61-2 | ¥1,930.00 | 询底价 |
50 mg | 1440898-61-2 | ¥3,950.00 | 询底价 |
100 mg | 1440898-61-2 | ¥6,370.00 | 询底价 |
5 mg | 1440898-61-2 | ¥738.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Deltarasin
描述: Deltarasin 是一种 KRAS-PDEδ 相互作用的小分子抑制剂,与纯化的 PDEδ 结合,Kd 值为 38 nM。
激酶实验: 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.
体外活性: 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]
体内活性: 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.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 93 mg/mL (154 mM)
DMSO : 93 mg/mL (154 mM)
关键字: Phosphodiesterase (PDE) | inhibit | Deltarasin | Inhibitor | Ras
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相关库: Anti-Prostate Cancer Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | GPCR Compound Library | Anti-Obesity Compound Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途