福他替尼|T6115

Fostamatinib
901119-35-5

询价 1removed 起订

上海更新日期：2026-05-08

TargetMol中国（陶术生物）

VIP14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：: 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：: 99.58%

产品类别：: 抑制剂

货号：: T001|T6115

Product Introduction

Bioactivity

名称	Fostamatinib
描述	Fostamatinib (R788) is a small-molecule inhibitor and an oral prodrug of R406, a Syk/FLT3-targeted inhibitor (IC50 = 41 nM) that also inhibits Lyn (IC50 = 63 nM) and Lck (IC50 = 37 nM), featuring oral activity and cell permeability, used for the treatment of immune thrombocytopenia.
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	方法：在体外实验中，从健康对照者分离的单核细胞与R406（fostamatinib活性代谢物，2 µM）共孵育24小时，进行红细胞吞噬及TNF-α产生测定。结果：R406显著降低单核细胞对IgG包被红细胞的吞噬（58.8%降至5.6%），并强烈抑制血红素或AIHA患者红细胞诱导的TNF-α产生。[1] 方法：采用HK、K30、TE1细胞，以10 μM Fostamatinib处理24-48 h，通过CCK-8、Transwell、划痕实验及Western blot检测。结果： Fostamatinib显著抑制细胞增殖、侵袭、迁移及LYN蛋白表达。[2]
体内活性	方法：在Louvain大鼠中单次口服给予Fostamatinib (R788) 10 mg/kg或20 mg/kg，检测其活性代谢物R406的血药浓度，计算药代动力学参数包括AUC0-16 hrs、Cmax和半衰期，并监测血浆中前药的存在情况。结果：R406在10 mg/kg和20 mg/kg剂量下的AUC0-16 hrs分别为10618 ng·h/mL和30650 ng·h/mL，Cmax分别为2600 ng/mL和6500 ng/mL（均在给药后1小时达到），半衰期均为4.2小时；血浆中未检测到前药R788，表明其完全转化为R406。[3]
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 \| 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 \| Acefylline \| Theobromine \| Sorafenib \| Pexidartinib \| Theophylline monohydrate \| Adenosine monophosphate \| Sulcatone \| Doxofylline
相关库	抗癌上市药物库 \| 已知活性化合物库 \| EMA 上市药物库 \| 激酶抑制剂库 \| 抗病毒库 \| FDA 上市药物库 \| GPCR靶点分子库 \| 膜蛋白靶向化合物库 \| 免疫/炎症分子化合物库 \| FDA 上市激酶抑制剂库 \| 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	(14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