Nintedanib (BIBF 1120)|656247-17-5|(尼达尼布; BIBF 1120)-陌孚医药/Medlife

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Nintedanib (BIBF 1120) (Synonyms: 尼达尼布; BIBF 1120)

目录号: PC16067 纯度: ≥98%

CAS No. :656247-17-5

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PC16067-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥891.00	请登录

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中文名称

Nintedanib (BIBF 1120)

中文别名

尼达尼布;尼达尼布 BIBF 1120;BIBF 1120靶向药;BIBF 1120固体状;BIBF 1120尼达尼布;BIBF 1120中间体;Nintedanib (BIBF 1120) 抑制剂;靶向药BIBF 1120;科研实验BIBF 1120;临床实验BIBF 1120;尼达尼布（BIBF-1120）;尼达尼布(Intedanib);尼达尼布-13C-D3(Intedanib-13C-D3);尼达尼布杂质;尼达尼布杂质对照品;抑制剂BIBF 1120

英文名称

Nintedanib (BIBF 1120)

英文别名

BIBF 1120;VARGATEF;INTEDANIB;Nintedanib;Nintedanib (BIBF 1120);(Z)-Methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)-phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate;[14C]-Intedanib;methyl (3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylate;Nintedanib (BIBF 1120,BIBF-1120 , Intedanib, Vargatef®);[14C]-Imidafenacin;3-[1-(4-{methyl-[2-(4-methyl-piperazin-1-yl)-acetyl]amino}phenylamino)-1-phenylmeth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indole-6-carb;3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone;4-(2-methyl-1-imidazolyl)-2,2-diphenylbutyramide;AC1O5FJP;BIBF-1120;Imidafenacin;Staybla;Staybla (TN);SureCN929680;Uritos;Uritos (TN);methyl (3Z)-3-{[(4-{methyl[(4-methylpiperazin-1-yl)acetyl]amino}phenyl)amino](phenyl)methylidene;BIBF1120;OFEV;(Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate;G6HRD2P839;Methyl (3z)-3-{[(4-{methyl[(4-Methylpiperazin-1-Yl)acetyl]amino}phenyl)amino](Phenyl)methyl

Cas No.

656247-17-5

分子式

C₃₁H₃₃N₅O₄

分子量

539.62

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

IC50 & Target[1][2]

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).

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

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

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res, 2008, 68(12), 4774-4782. [Information]

[2]. Roth GJ, et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). J Med Chem, 2009, 52(14), 4466-4480. [Information]

溶解度数据

体外研究:

DMSO : 11.5 mg/mL (21.31 mM; Need ultrasonic)

配制储备溶液

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
10 mM	0.1853 mL	0.9266 mL	1.8532 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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