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网站主页 化工产品目录 生物化工 抑制剂 血管生成(Angiogenesis) Syk 抑制剂 福他替尼 福他替尼
  • 福他替尼|T6115

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:2025-10-31

TargetMol中国(陶术生物)

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联系人:邵小姐
电话:021-021-33632979拨打
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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:
store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
纯度规格:
99.38%
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store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 127.5 mg/mL (219.65 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (6.89 mM), Sonication is recommended.
关键字Syk | Spleen tyrosine kinase | R-788 | R 788 | MonoamineTransporter | Monoamine Transporter | Monoamine transporter | Inhibitor | inhibit | Fostamatinib | Fms like tyrosine kinase 3 | FLT3 | Cluster of differentiation antigen 135 | CD135 | AdenosineReceptor | Adenosine transporter | Adenosine Receptor | A3
相关产品Inosine | Gilteritinib | ANTHRAQUINONE-2-CARBOXYLIC ACID | Theophylline | Adenosine 5'-monophosphate disodium salt | Acefylline | Theobromine | Sorafenib | Theophylline monohydrate | Adenosine monophosphate | Sulcatone | Doxofylline
相关库抑制剂库 | 抗癌上市药物库 | 已知活性化合物库 | EMA 上市药物库 | FDA 上市药物库 | 抗病毒库 | GPCR靶点分子库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | FDA 上市激酶抑制剂库 | 酪氨酸激酶分子库 | 抗癌临床化合物库
福他替尼|||R788|TargetMol

公司简介

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 (13年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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