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Entospletinib

Entospletinib

产品编号 T6101   CAS 1229208-44-9
别名: GS-9973

Entospletinib (GS-9973) 是选择性的Syk 抑制剂,其IC50=7.7 nM。

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Entospletinib Chemical Structure
Entospletinib, CAS 1229208-44-9
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 待询
200 mg ¥ 5,460 待询
1 mL * 10 mM (in DMSO) ¥ 575 现货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Entospletinib (T6101)
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选择批次  
纯度: 99.51%
纯度: 99.05%
纯度: 98.2%
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生物活性
化学信息
存储 & 溶解度
参考文献
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 In cells, GS-9973 also displays excellent specificity for Syk, and effectively inhibits BCR-mediated activation and proliferation of B-cells, as well as immune-complex-stimulated cytokine production in monocytes. In Caco-2 cell, GS-9973 exhibits good bidirectional permeability across cell monolayers.
体内活性 In rat and dog, GS-9973 (1 mg/kg) by oral administration shows moderate to high bioavailability. In a rat collagen-induced arthritis model, GS-9973 (1-10 mg/kg) by oral administrations significantly suppress ankle inflammation. GS-9973(ED50 =1.2 -3.9 mg/kg) exhibits disease-modifying activity such as pannus formation, cartilage damage, bone resorption, and periosteal bone formation.
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (121.52 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. J Med Chem. 2014, 57(9), 3856-3873. 2. Burke RT, et al. Oncotarget. 2014, 5(4), 908-915.

TargetMol Library Books文献引用

1. Geng R, Zhao Y, Xu W, et al.SIRPB1 regulates inflammatory factor expression in the glioma microenvironment via SYK: functional and bioinformatics insights.Journal of Translational Medicine.2024, 22(1): 338
Cerdulatinib Gusacitinib Cevidoplenib dimesylate PRT062607 hydrochloride URMC-099 TAS05567 Sovleplenib Syk Inhibitor II

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗癌上市药物库 酪氨酸激酶分子库 抗癌活性化合物库 激酶抑制剂库 抗癌药物库 抗癌临床化合物库 药物功能重定位化合物库 FDA 上市激酶抑制剂库 口服活性化合物库

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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。

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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。

Keywords

Entospletinib 1229208-44-9 Angiogenesis Tyrosine Kinase/Adaptors Syk inhibit Spleen tyrosine kinase GS-9973 GS 9973 GS9973 Inhibitor inhibitor

 

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