Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 428 | 现货 | ||
2 mg | ¥ 622 | 现货 | ||
5 mg | ¥ 1,230 | 现货 | ||
10 mg | ¥ 1,950 | 现货 | ||
25 mg | ¥ 3,370 | 现货 | ||
50 mg | 特惠询价 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,650 | 现货 |
产品描述 | Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
靶点活性 | PDEδ:38 nM(Kd) |
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. |
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. |
分子量 | 603.75 |
分子式 | C40H37N5O |
CAS No. | 1440898-61-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 93 mg/mL (154 mM)
DMSO: 93 mg/mL (154 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.6563 mL | 8.2816 mL | 16.5631 mL | 41.4079 mL |
5 mM | 0.3313 mL | 1.6563 mL | 3.3126 mL | 8.2816 mL | |
10 mM | 0.1656 mL | 0.8282 mL | 1.6563 mL | 4.1408 mL | |
20 mM | 0.0828 mL | 0.4141 mL | 0.8282 mL | 2.0704 mL | |
50 mM | 0.0331 mL | 0.1656 mL | 0.3313 mL | 0.8282 mL | |
100 mM | 0.0166 mL | 0.0828 mL | 0.1656 mL | 0.4141 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Deltarasin 1440898-61-2 GPCR/G Protein MAPK Metabolism PDE Ras Phosphodiesterase (PDE) inhibit Inhibitor inhibitor