2. Protein Tyrosine Kinase/RTK
  3. PDGFR VEGFR FGFR
  4. Nintedanib

Nintedanib  (Synonyms: 尼达尼布; BIBF 1120)

目录号: HY-50904 纯度: 99.90%
COA 产品使用指南

摩尔计算器

Nintedanib (BIBF 1120) 是一种有效的三重血管激酶抑制剂，抑制 VEGFR1/2/3，FGFR1/2/3 和 PDGFRα/β 的 IC50 值分别为 34 nM/13 nM/13 nM，69 nM/37 nM/108 nM 和 59 nM/65 nM。

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Nintedanib Chemical Structure

Nintedanib Chemical Structure

CAS No. : 656247-17-5

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥712
In-stock
5 mg ￥600
In-stock
10 mg ￥900
In-stock
50 mg ￥2450
In-stock
100 mg ￥3450
In-stock
200 mg ￥4850
In-stock
500 mg 现货 询价
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Nintedanib:

Nintedanib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 48 篇科研文献

WB
Proliferation Assay

    Nintedanib purchased from MCE. Usage Cited in: Sci Rep. 2018 Jun 22;8(1):9540.  [Abstract]

    Western blot based detection of cell cycle associated molecules viz., Cyclins A, D1 and E, and CDKs 2, 4 and 6 in PC3, and LNCaP cells after 72 hours of Nintedanib treatment.

    Nintedanib purchased from MCE. Usage Cited in: Oncol Rep. 2016 Dec;36(6):3123-3130.  [Abstract]

    The mice are treated with TFTD alone (150 mg/kg, orally twice daily from days 1 to 14, open column), or a combination of TFTD and Nintedanib (closed column). The HT-29 and HCT116 tumors are collected at 24 h following the final administration of the drugs (day 15). The values indicate the mean ± SD (n=6).

    查看 PDGFR 亚型特异性产品:

    查看所有亚型
    PDGFR PDGFRβ PDGFRα

    查看 VEGFR 亚型特异性产品:

    查看所有亚型
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    查看 FGFR 亚型特异性产品:

    查看所有亚型
    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

    IC50 & Target[1]

    VEGFR1

    34 nM (IC50)

    VEGFR2

    13 nM (IC50)

    VEGFR3

    13 nM (IC50)

    FGFR1

    69 nM (IC50)

    FGFR2

    37 nM (IC50)

    FGFR3

    108 nM (IC50)

    PDGFRα

    59 nM (IC50)

    PDGFRβ

    65 nM (IC50)

    体外研究
    (In Vitro)

    Nintedanib (BIBF 1120) binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. Nintedanib (BIBF 1120) inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. Nintedanib (BIBF 1120) (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. Nintedanib (BIBF 1120) prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC)[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Nintedanib 相关抗体:
    体内研究
    (In Vivo)

    Nintedanib (BIBF 1120) (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[1]. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    539.62

    Formula

    C31H33N5O4
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    尼达尼布
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 5.83 mg/mL (10.80 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8532 mL 9.2658 mL 18.5316 mL
    5 mM 0.3706 mL 1.8532 mL 3.7063 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (18.53 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂： 1% CMC/0.5% Tween-80 in Saline water

      Solubility: 10 mg/mL (18.53 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.94%

    COA (197 KB) HNMR (281 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [2]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Nintedanib 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8532 mL 9.2658 mL 18.5316 mL 46.3289 mL
    5 mM 0.3706 mL 1.8532 mL 3.7063 mL 9.2658 mL
    10 mM 0.1853 mL 0.9266 mL 1.8532 mL 4.6329 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Nintedanib656247-17-5BIBF 1120尼达尼布BIBF1120BIBF-1120PDGFRVEGFRFGFRPlatelet-derived growth factor receptorVascular endothelial growth factor receptorFibroblast growth factor receptorInhibitorinhibitorinhibit

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