乙磺酸尼达尼布|T5001|TargetMol

Nintedanib esylate
656247-18-6

￥108 1mg 起订

￥198 5mg 起订

￥322 10mg 起订

上海更新日期：2026-02-25

TargetMol中国（陶术生物）

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联系人：邵小姐

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产品详情:

中文名称：: 乙磺酸尼达尼布

英文名称：: Nintedanib esylate

CAS号：: 656247-18-6

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from direct sunlight,keep away from moisture,store at low temperature,store under nitrogen | 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：: 99.98%

产品类别：: 抑制剂

货号：: T5001

Product Introduction

Bioactivity

名称	Nintedanib esylate
描述	Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β
激酶实验	Enzyme activity is assayed in the presence or absence of serial dilutions of BIBF1120 performed in 25% DMSO. Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound. All incubations are conducted at room temperature on a rotation shaker. 10 μL of each BIBF1120 dilution is added to 10 μL of diluted kinase (0.8 μg/mL VEGFR2, 10 mM Tris pH 7.5, 2 mM EDTA, and 2 mg/mL BSA) and preincubated for 1 hour. The reaction is started by addition of 30 μL of substrate mix containing 62.4 mM Tris pH 7.5, 2.7 mM DTT, 5.3 mM MnCl2, 13.3 mM Mg-acetate, 0.42 mM ATP, 0.83 mg/mL Poly-Glu-Tyr(4:1), and 1.7 μg/mL Poly-Glu-Tyr(4:1)-biotin and incubated for 1 hour. The reaction is stopped by addition of 50 μL of 250 mM EDTA, 20 mM HEPES, pH 7.4. 90 μL of the reaction mix is transferred to a streptavidin plate and incubated for 1-2 hours. After three washes with PBS the EU-labeled antibody, PY20 is added (recommended dilution 1:2000 of 0.5 mg/mL labeled antibody in DELFIA assay buffer). Excessive detection antibody is removed by three ishes of DELFIA washing buffer. Then 10 minutes before measurement on the multilabel reader, each well is incubated with 100 μL of DELFIA enhancement solution.
动物实验	Five-week-old to 6-wk-old athymic NMRI-nu/nu female mice (21-31 g) are used for the assay. After acclimatization, mice are inoculated with 1 to 5×106 (in 100 μL) FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 cells s.c. into the right flank of the animal. After acclimatization, F344 Fischer rats are injected with 5×106 (in 100 μL) GS-9L cells s.c. into the right flank of the animal. For pharmacokinetic analysis, blood is isolated at indicated time points from the retroorbital plexus of mice and plasma is analyzed using high performance liquid chromatography-mass spectrometry methodology.
体外活性	BIBF 1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC).
体内活性	BIBF1120 (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition. BIBF1120 is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated.
存储条件	keep away from direct sunlight,keep away from moisture,store at low temperature,store under nitrogen \| 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 : 101 mg/mL (155.44 mM), Sonication is recommended.
关键字	VEGFR3 \| VEGFR2 \| VEGFR1 \| VEGFR \| PDGFRβ \| PDGFRα \| PDGFR \| Nintedanib esylate \| Nintedanib \| FGFR3 \| FGFR2 \| FGFR1 \| FGFR \| esylate \| BIBF-1120 \| BIBF1120
相关产品	glycine \| Amlexanox \| Lenvatinib \| Formononetin \| Thymoquinone \| Ferulic Acid \| Regorafenib \| Pazopanib \| Ethyl cinnamate \| Sorafenib \| Regorafenib monohydrate \| Albendazole
相关库	抑制剂库 \| 抗癌上市药物库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| EMA 上市药物库 \| FDA 上市药物库 \| 膜蛋白靶向化合物库 \| 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

乙磺酸尼达尼布|||Nintedanib Ethanesulfonate Salt|||BIBF 1120 (esylate)|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	(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