福他替尼|T6115

Fostamatinib
901119-35-5

￥345 1mg 起订

￥493 2mg 起订

￥828 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 福他替尼

英文名称：: Fostamatinib

CAS号：: 901119-35-5

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.3%

产品类别：: 抑制剂

货号：: T6115

Product Introduction

Bioactivity

名称	Fostamatinib
描述	Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.
细胞实验	Cultured human mast cells (CHMC) are derived from cord blood CD34+ progenitor cells and grown, primed, and stimulated and shown in supplemental data. Before stimulation, cells are incubated with R788 or DMSO for 30 minutes. Cells are then stimulated with either 0.25 to 2 mg/mL anti-IgE or anti-IgG or 2 μM ionomycin. For tryptase measurement, ∼1500 cells per well are stimulated for 30 min in modified Tyrode's buffer. For LTC4 and cytokine production, 100,000 cells per well are stimulated for 1 or 7 hours, respectively. Tryptase activity is measured by luminescence readout of a peptide substrate, and LTC4 and cytokines are measured using Luminex multiplex technology. (Only for Reference)
激酶实验	Fluorescence polarization kinase assay and Ki determination: The fluorescence polarization reactions are performed. For Ki determination, duplicate 200-μL reactions are set up at eight different ATP concentrations from 200 μM (2-fold serial dilutions) in the presence of either DMSO or R788 at 125, 62.5, 31.25, 15.5, or 7.8 nM. At different time points, 20 μL of each reaction is removed and quenched to stop the reaction. For each concentration of R788, the rate of reaction at each concentration of ATP is determined and plotted against the ATP concentration to determine the apparent Km and Vmax (maximal rate). Finally the apparent Km (or apparent Ki/Vmax) is plotted against the inhibitor concentration to determine the Ki.
体外活性	在风湿性关节炎模型中,Fostamatinib 明显减少炎症介质,比如TNFalpha,IL-1,IL-6和IL-18,从而减少炎症和骨退化.Fostamatinib 能够有效抑制体内BCR信号,导致恶性B细胞的增殖和存活减少,并明显延长治疗组动物的存活.在逆转-被动阿瑟斯反应和双抗体诱导的关节炎小鼠模型中,口服Fostamatinib减少免疫复合物介导的炎症.
体内活性	在人肥大细胞,巨噬细胞,和中性粒细胞中,Fostamatinib能够特异性抑制FcγR信号。在大部分DLBCL细胞系,Fostamatinib诱导细胞凋亡。Fostamatinib（EC50 =56 nM）以剂量依赖方式抑制抗- IgE介导的CHMC脱粒,它也会抑制抗-IgE诱导的LTC4,细胞因子以及趋化因子,包括TNFα,IL-8,和GM-CSF的产生与释放。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 107 mg/mL (184.3 mM)
关键字	Inhibitor \| Spleen tyrosine kinase \| Cluster of differentiation antigen 135 \| Fms like tyrosine kinase 3 \| CD135 \| inhibit \| Fostamatinib \| FLT3 \| Syk \| R 788 \| R-788
相关产品	Adenosine 5'-monophosphate monohydrate \| Inosine \| Gilteritinib \| ANTHRAQUINONE-2-CARBOXYLIC ACID \| Theophylline \| Acefylline \| Theobromine \| Nintedanib \| Sorafenib \| Theophylline monohydrate \| Diphylline \| Doxofylline
相关库	经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗病毒库 \| FDA 上市药物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库

福他替尼|||R788|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
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