Name: Nintedanib
Brand: TargetMol
SKU: T1777
Price: 207 CNY
Availability: InStock
Rating: 5 (10 reviews)

Nintedanib

很棒

产品编号 T1777Cas号 656247-17-5

别名 尼达尼布, Intedanib, BIBF 1120

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。

规格

价格

库存

数量

1 mg

¥ 207

In stock

5 mg

¥ 459

In stock

10 mg

¥ 702

In stock

25 mg

¥ 1,220

In stock

50 mg

¥ 1,880

In stock

100 mg

¥ 2,720

In stock

200 mg

¥ 3,750

In stock

1 mL x 10 mM (in DMSO)

¥ 559

In stock

产品介绍

生物活性

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	FGFR2:37 nM (cell free), FGFR1:69 nM (cell free), VEGFR3:13 nM (cell free), FGFR3:108 nM, PDGFRα:59 nM (cell free), VEGFR1:34 nM (cell free), PDGFRβ:65 nM, 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	尼达尼布, Intedanib, BIBF 1120

化学信息

分子量	539.62
分子式	C₃₁H₃₃N₅O₄
CAS No.	656247-17-5
Smiles	COC(c1cc2c(/C(C(N2)=O)=C(c3ccccc3)/Nc4ccc(N(C(CN5CCN(CC5)C)=O)C)cc4)cc1)=O
密度	1.284 g/cm3 (Predicted)

储存&溶解度

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

Ethanol: 3 mg/mL (5.56 mM), Sonication is recommended.

DMSO: 13.1 mg/mL (24.28 mM), Sonication and heating are recommended.

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

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 0.6 mg/mL (1.11 mM), Solution.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8532 mL	9.2658 mL	18.5316 mL	92.6578 mL
5 mM	0.3706 mL	1.8532 mL	3.7063 mL	18.5316 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.1853 mL	0.9266 mL	1.8532 mL	9.2658 mL
20 mM	0.0927 mL	0.4633 mL	0.9266 mL	4.6329 mL

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 ， TargetMol | Animal experiments

一共给药动物 10 只 ，您使用的配方为 5% TargetMol | reagent

DMSO+ 30%PEG300+ 5%Tween 80 + 60%Saline/PBS/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 μLDMSO TargetMol | reagent

（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 50μLDMSO TargetMol | reagent

母液，添加 300 μLPEG300 TargetMol | reagent

混匀澄清，再加 50μLTween 80, 混匀澄清，再加 600μLSaline/PBS/ddH₂O TargetMol | reagent

混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

Nintedanib

Nintedanib

产品介绍

化合物与蛋白结合的复合物

计算器

体内实验配液计算器

剂量转换

SCI 文献

关键词

评论列表