| 名称 | Entospletinib |
| 描述 | Entospletinib (GS-9973) is a Syk inhibitor (IC50=7.7 nM) with selective, oral activity. Entospletinib has potential value in the treatment of a variety of hematological malignancies and immune-related diseases. |
| 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. |
| 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. |
| 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. |
| 体外活性 | 方法：NALM-6和SEM细胞系用Entospletinib（1、5、10 μM）处理72小时，使用Western Blot方法检测靶蛋白表达水平。
结果：Entospletinib显著影响了pAKT、pERK、pGSK3β、p53和BCL-6等关键蛋白的表达。[1] |
| 体内活性 | 方法：为研究Entospletinib的抗炎活性，将Entospletinib（100 mg/kg）口服给K/BxN血清诱导的关节炎小鼠，每日两次。
结果：Entospletinib显著减轻了关节炎症的宏观表现，包括关节肿胀和临床评分。[2]
方法：为研究Entospletinib的抗炎活性，将Entospletinib（10 mg/kg）口服给大鼠CIA模型。
结果：Entospletinib表现出显著的抗炎效果。[3] |
| 存储条件 | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 50 mg/mL (121.52 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 2.5 mg/mL (6.08 mM), Sonication is recommeded.
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| 关键字 | Syk | Spleen tyrosine kinase | Inhibitor | inhibit | GS9973 | GS 9973 | Entospletinib |
| 相关产品 | Cerdulatinib hydrochloride | Syk-IN-3 | ANTHRAQUINONE-2-CARBOXYLIC ACID | Piceatannol | Ellagic acid | GSK1904529A | URMC-099 | Cerdulatinib | Gusacitinib | R112 | TC-S 7003 | PRT062607 hydrochloride |
| 相关库 | 抑制剂库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 激酶抑制剂库 | 膜蛋白靶向化合物库 | 免疫/炎症分子化合物库 | 药物功能重定位化合物库 | 酪氨酸激酶分子库 | FDA 上市激酶抑制剂库 | 抗癌临床化合物库 | 抗癌药物库 |