|Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Entospletinib (GS-9973) 是选择性的Syk 抑制剂,其IC50=7.7 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 239 | 现货 | ||
2 mg | ¥ 335 | 现货 | ||
5 mg | ¥ 519 | 现货 | ||
10 mg | ¥ 847 | 现货 | ||
25 mg | ¥ 1,530 | 现货 | ||
50 mg | ¥ 2,580 | 现货 | ||
100 mg | ¥ 3,870 | 现货 | ||
200 mg | ¥ 5,460 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 575 | 现货 |
产品描述 | Entospletinib (GS-9973) (IC50= 7.7 nM)is a specific Syk inhibitor, which is orally bioavailable. |
靶点活性 | Syk:IC50: 7.7 nM |
体外活性 | 在细胞内,GS-9973对Syk展现出极高的特异性,并有效抑制BCR介导的B细胞激活与增殖,同时抑制免疫复合物刺激的单核细胞中的细胞因子产生。在Caco-2细胞中,GS-9973显示出良好的双向跨细胞单层的渗透性。 |
体内活性 | 在大鼠和狗的实验中,通过口服给予Entospletinib (1 mg/kg) 显示出中等至高的生物利用度。在大鼠胶原诱导的关节炎模型中,Entospletinib (1-10 mg/kg) 通过口服给药明显抑制踝部炎症。Entospletinib(ED50=1.2-3.9 mg/kg) 表现出改变疾病进程的活性,如滑膜炎形成、软骨损伤、骨吸收及骨膜下骨形成等。 |
激酶实验 | In the determination of full-length baculovirus expressed Syk kinase activity, the reaction system was 25 μL containing 25 mM Tris-HCl, pH 7.5, 5 mM β-glycerophosphate, 2 mM DTT, 0.1 mM Na3VO4, 10 mM MgCl2, 0.5 μM Promega PTK Biotin Peptide Substrate 1, 0.01% casein, 1, 0.01% Triton X-100, 0.25% Glycerol, and 40 mM ATP (Km for ATP). After incubation for 60 minutes at room temperature, the reaction was stopped by adding 30 mM EDTA (30 μL of SA-APC and 4 nM PT-66 antibody). After measuring the plate, the IC50 value of the test compound was calculated using a 4-parameter linear regression algorithm. |
细胞实验 | In MV-4-11 cells, the functional effect of the compound on the cellular Flt3 activity was determined by inhibition of cell proliferation. Cells were diluted in 96 well flat bottom tissue culture plates in RPMI medium containing 10% FBS and compound dilutions were added and incubated at 37°C for 72 hours. Aramazol (10%) was added to the cells and the cells were incubated for another 12-18 hours at 37°C. Finally, the inhibition of the relative cell number was measured at 570/600 nm in the spectrophotometer. |
动物实验 | In the rat collagen-induced arthritis (CIA) model, Entospletinib (10 mg/kg), which is dissolved in hydrogenated castor oil,ethanol or physiological saline, is taken by oral. |
别名 | GS-9973 |
分子量 | 411.46 |
分子式 | C23H21N7O |
CAS No. | 1229208-44-9 |
|Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (121.52 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4304 mL | 12.1518 mL | 24.3037 mL | 60.7592 mL |
5 mM | 0.4861 mL | 2.4304 mL | 4.8607 mL | 12.1518 mL | |
10 mM | 0.243 mL | 1.2152 mL | 2.4304 mL | 6.0759 mL | |
20 mM | 0.1215 mL | 0.6076 mL | 1.2152 mL | 3.038 mL | |
50 mM | 0.0486 mL | 0.243 mL | 0.4861 mL | 1.2152 mL | |
100 mM | 0.0243 mL | 0.1215 mL | 0.243 mL | 0.6076 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。
Entospletinib 1229208-44-9 Angiogenesis Tyrosine Kinase/Adaptors Syk inhibit Spleen tyrosine kinase GS-9973 GS 9973 GS9973 Inhibitor inhibitor