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Nintedanib

Nintedanib

产品编号 T1777   CAS 656247-17-5
别名: BIBF 1120, Intedanib, 尼达尼布

Nintedanib (Intedanib) 是一种三重血管激酶抑制剂,抑制 VEGFR1、VEGFR2、VEGFR3 (IC50=34/13/13 nM),FGFR1、FGFR2、FGFR3 (IC50=69/37/108 nM),PDGFRα、PDGFRβ (IC50=59/65 nM)。Nintedanib 具有抗肿瘤活性,通过抑制血管生成来抑制肿瘤生长。

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Nintedanib Chemical Structure
Nintedanib, CAS 656247-17-5
规格 价格/CNY 货期 数量
1 mg ¥ 218 现货
5 mg ¥ 483 现货
10 mg ¥ 739 现货
25 mg ¥ 1,290 现货
50 mg ¥ 1,980 现货
100 mg ¥ 2,870 现货
200 mg ¥ 3,950 现货
500 mg ¥ 6,980 现货
1 mL * 10 mM (in DMSO) ¥ 588 现货
其他形式的 Nintedanib:
产品目录号及名称: Nintedanib (T1777)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/108 nM), PDGFRα, and PDGFRβ (IC50=59/65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.
靶点活性 PDGFRα:59 nM (cell free), FGFR1:69 nM (cell free), FGFR2:37 nM (cell free), VEGFR1:34 nM (cell free), VEGFR3:13 nM (cell free), VEGFR2:13 nM (cell free)
体外活性 方法:人鼻咽癌细胞 CNE-2、HNE-1 和 HONE-1 用 Nintedanib (0.078-10 µM) 处理 72 h,使用 CCK8 assay 检测细胞活力。
结果:Nintedanib 以剂量依赖的方式显著抑制 CNE-2、HNE-1 和 HONE-1 细胞系的生长,IC50 值分别为 4.16 µM、5.62 µM 和 6.32 µM。[1]
方法:人内皮细胞 HUVEC、平滑肌细胞 HUASMC 和牛视网膜周细胞用 Nintedanib (0.03-1 µM) 处理 2 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:Nintedanib 抑制 HUVEC、HUASMC 和牛视网膜周细胞中 MAPK 和 Akt 的配体依赖性磷酸化。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Nintedanib (10-100 mg/kg) 灌胃给药给携带人头颈部小细胞癌肿瘤 FaDu 或人肾癌肿瘤 Caki-1 的 athymic NMRI-nu/nu 小鼠,每天一次,持续 23-35 天。
结果:Nintedanib 抑制 FaDu 和 Caki-1 的肿瘤生长。[2]
方法:为检测体内抗肿瘤活性,将 Nintedanib (40 mg/kg) 和 TFTD (150 mg/kg) 腹腔注射给携带肿瘤 DLD-1、DLD-1/5-FU、HT-29 或 HCT116 的 BALB/c nu/nu 小鼠,每天两次,持续两周。
结果:在第 15 天,Nintedanib 和 TFTD 单药治疗疗导致体内肿瘤生长显著减少。联合疗法表现出比两种单一疗法更大的抗肿瘤活性。[3]
激酶实验 The cytoplasmic tyrosine kinase domain of VEGFR-2 (residues 797–1355 according to sequence deposited in databank SWISS-PROT P35968) was cloned into pFastBac fused to GST and extracted as described in supplementary methods. Enzyme activity was assayed using standard conditions using a random polymer (Glu/Tyr 4:1) and in the presence of 100 μmol/L ATP (for details, see supplementary methods). For all other kinase assays, the entire cytoplasmic domains of the receptors (from the end of the transmembrane to the COOH terminus) were cloned into pFastBac vector containing GST and assayed under standard conditions [1].
细胞实验 HUVEC, HUASMC, and BRP were cultured as described above. Two hours before the addition of ligands, BIBF 1120 was added to the cultures. Cell lysates were generated according to standard protocols. Western blotting was done using standard SDS-PAGE methods, loading 50 to 75 μg of protein per lane, with detection by enhanced chemiluminescence. Total and phosphorylated mitogen-activated protein kinase (MAPK) was analyzed using monoclonal antibodies M3807 and M8159. Total Akt was detected using the polyclonal antibody and phosphorylated Akt (Ser473) was analyzed with the monoclonal antibody. Cleaved caspase-3 was detected with the monoclonal antibody [1].
动物实验 Five-week-old to 6-wk-old athymic NMRI-nu/nu female mice (21–31 g) were purchased from Harlan. After acclimatization, mice were inoculated with 1 to 5 × 10^6 (in 100 μL) FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 cells s.c. into the right flank of the animal. F344 Fischer rats after acclimatization were injected with 5 × 10^6 (in 100 μL) GS-9L cells s.c. into the right flank of the animal. For pharmacokinetic analysis, blood was isolated at indicated time points from the retroorbital plexus of mice and plasma was analyzed using high-performance liquid chromatography-mass spectrometry methodology [1].
别名 BIBF 1120, Intedanib, 尼达尼布
化合物与蛋白结合的复合物

T1777_1

STRUCTURE OF RET PROTEIN TYROSINE KINASE DOMAIN IN COMPLEX WITH NINTEDANIB

分子量 539.62
分子式 C31H33N5O4
CAS No. 656247-17-5

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 3 mg/mL (5.55 mM)

DMSO: 6 mg/mL (11.11 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / 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
DMSO 10 mM 0.1853 mL 0.9266 mL 1.8532 mL 4.6329 mL

计算器

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分子量计算器
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参考文献

1. Xue C, et al. Efficacy of BIBF 1120 or BIBF 1120 plus chemotherapy on nasopharyngeal carcinoma in vitro and in vivo. Drug Des Devel Ther. 2016 Mar 15;10:1173-80. 2. Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. 3. Suzuki N, et al. Effect of a novel oral chemotherapeutic agent containing a combination of trifluridine, tipiracil and the novel triple angiokinase inhibitor nintedanib, on human colorectal cancer xenografts. Oncol Rep. 2016 Dec;36(6):3123-3130.

文献引用

1. Dong X, Wang L, Wang D, et al.Proteomic study on nintedanib in gastric cancer cells.PeerJ.2024, 12: e16771.
ENMD-2076 Sunitinib GZD856 PD-089828 ON123300 SU14813 R1530 Ripretinib

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 酪氨酸激酶分子库 抗癌上市药物库 抗癌药物库 儿童药物库 FDA 上市激酶抑制剂库 上市药物库 HIF-1化合物库 NO PAINS 化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Nintedanib 656247-17-5 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR FLT PDGFR Src BIBF 1120 Inhibitor Platelet-derived growth factor receptor Fibroblast growth factor receptor Vascular endothelial growth factor receptor Intedanib 尼达尼布 BIBF1120 inhibit BIBF-1120 inhibitor

 

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