Nintedanib

别名: BIBF 1120, Intedanib 中文名称：尼达尼布

目录号：S1010 Purity: 99.98%

Nintedanib尼达尼布是一种有效的三重血管激酶抑制剂，作用于VEGFR1/2/3， FGFR1/2/3和PDGFRα/β，在无细胞试验中IC50分别为34 nM/13 nM/13 nM， 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。

Nintedanib Chemical Structure

CAS: 656247-17-5

规格	价格	库存
10mM (1mL in DMSO)	RMB 1970.51	现货
5mg	RMB 991.25	现货
50mg	RMB 5492.96	现货
200mg	RMB 10401.3	现货
1g	RMB 14496.3	现货
更大包装有超大折扣
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客户使用Selleck的Nintedanib发表文献138篇

产品质控

批次：纯度： 99.98%

99.98

Nintedanib相关产品

相关靶点	VEGFR1 VEGFR2 VEGFR3	点击展开
相关化合物库	激酶抑制剂库酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库细胞周期化合物库血管生成相关化合物库	点击展开

VEGFR抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
PLC5	Cell Viability Assay	0-20 μM	48 h	decreases cell viability dose dependently	24657398
HepG2	Cell Viability Assay	0-20 μM	48 h	decreases cell viability dose dependently	24657398
Hep3B	Cell Viability Assay	0-20 μM	48 h	decreases cell viability dose dependently	24657398
A549	Function Assay	5 μM	0-1 h	increases AP-1 activation after 30 min	25843005
A549	Function Assay	0.01–5 μM	72 h	enhances SP-D protein expression in a dose-dependent manner at concentrations of up to 5 μM	25843005
A549	Function Assay	0.01–5 μM	24 h	induces SFTPD mRNA expression dose dependently	25843005
Mia-Paca2	Function Assay	2/5 μM	24 h	has a general EMT reversal effect	26061747
T24	Function Assay	2/5 μM	24 h	has a general EMT reversal effect	26061747
A549	Function Assay	2/5 μM	24 h	has a general EMT reversal effect	26061747
SKOV3	Function Assay	5 µM	24 h	induces a significant increase in the promoter activities of E-cad, CDH1, and CDH3	26061747
HuH7	Cell Viability Assay	0-20 μM	48 h	decreases cell viability dose dependently	24657398
SK-Hep1	Cell Viability Assay	0-20 μM	48 h	decreases cell viability dose dependently	24657398
Hep3B	Apoptosis Assay	0-20 μM	48 h	induces cell apoptosis dose dependently	24657398
HepG2	Apoptosis Assay	0-20 μM	48 h	induces cell apoptosis dose dependently	24657398
PLC5	Apoptosis Assay	0-20 μM	48 h	induces cell apoptosis dose dependently	24657398
HuH7	Apoptosis Assay	0-20 μM	48 h	induces cell apoptosis dose dependently	24657398
SK-Hep1	Apoptosis Assay	0-20 μM	48 h	induces cell apoptosis dose dependently	24657398
NIH3T3	Function assay	50 nM	1 hr	Inhibition of VEGFR2 transfected in mouse NIH3T3 cells at 50 nM incubated for 1 hr measured after 32 hrs washout followed by VEGF stimulation for 10 mins by Western blotting	18559524
Sf9	Function assay		20 mins	Inhibition of mouse GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting, IC50 = 0.013 μM.	18559524
Sf9	Function assay		20 mins	Inhibition of human GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting, IC50 = 0.021 μM.	18559524
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 4.9 μM.	28190652
SKOV3	Antiproliferative assay		72 hrs	Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay, IC50 = 28.76 μM.	28190652
BL21 (DE3)	Function assay		30 mins	Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method, Ki = 0.0056 μM.	28351607
BL21 (DE3)	Function assay		30 mins	Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method, IC50 = 0.043 μM.	28351607
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.83 μM.	28826084
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 8.28 μM.	28826084
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 22.62 μM.	28826084
NIH/3T3	Function assay		42 hrs	Inhibition of PDGFR in mouse NIH/3T3 cells assessed as reduction in recombinant human PDGF-BB-induced cell proliferation after 42 hrs by cell titer 96 aqueous one solution based assay, IC50 = 0.085 μM.	29152045
NIH3T3	Function assay		1 hr	Inhibition of VEGF-stimulated human VEGFR2 phosphorylation expressed in mouse NIH3T3 cells pretreated for 1 hr measured 32 hrs after drug dose by immunoprecipitation based pulse-chase experiment	19522465
H1703	Growth Inhibition Assay			IC50=0.05 μM	23729403
Sf9	Function assay			Inhibition of human VEGFR2 expressed in Sf9 cells, IC50 = 0.005 μM.	19522465
BRP	Apoptosis assay			Induction of apoptosis in BRP cells assessed as caspase-3 cleavage	19522465
BRP	Antiangiogenic assay			Antiangiogenic activity BRP cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay	19522465
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
点击查看更多细胞系数据

生物活性

产品描述

靶点

VEGFR2 ^[1] (Cell-free assay)	VEGFR3 ^[1] (Cell-free assay)	LCK ^[1] (Cell-free assay)	FLT3 ^[1] (Cell-free assay)	VEGFR1 ^[1] (Cell-free assay)	点击更多
13 nM	13 nM	16 nM	26 nM	34 nM	点击更多

体外研究(In Vitro)
体外研究活性	BIBF1120对酪氨酸激酶受体如EGFR, HER2, InsR, IGF1R 或者细胞周期激酶 CDK1, CDK2 和CDK4抑制效果不大， IC50都大于1x10³nM。BIBF1120强抑制VEGF-刺激的HUVEC 和VEGF-刺激的HSMEC，EC50分别为9 和 7 nM。相反，BIBF1120 作用于FaDu, Calu-6 和Hela时EC50则大到几百倍。^[1]
激酶实验	激酶实验
激酶实验	VEGFR-2的胞质酪氨酸激酶域克隆到pFastBac载体上，与谷胱甘肽巯基转移酶 (GST)相融合。 GST融合蛋白在SF-9昆虫细胞中表达，用重元素萃取分离法提取。HEPEX萃取液包括20 mM HEPES （pH 为7.4）, 100 mM NaCl, 10 mM ss-甘油磷酸盐, 10 mM 聚硝基磷酸单苯酯, 30mM NaF, 5 mM EDTA, 5% 甘油, 1% Triton X-100, 1 mM Na₃VO₄, 0.1% SDS, 0.5μg/ml 抑肽素A, 2.5 μg/ml 3,4-二氯异香豆素(丝氨酸蛋白酶的不可逆抑制剂), 2.5 μg/ml反式-环氧琥珀酰-L-亮氨酰-L-氨基丁烷, 20 KIU/ml 抑肽酶, 2 μg/ml 亮抑肽酶, 1 mM苯甲脒，和0.002% PMSF。谷氨酸和酪氨酸按4:1比例随机组成的聚合物作为基底物，每组50ul的反应液包括5 % DMSO, 40 mM HEPES （pH 为 7.4）, 5 mM MgCl₂, 5 mM MnCl₂, 0.5 mg/ml 聚谷氨酸/酪氨酸, 0.05% Triton X-100, 100 μM ATP, 1 μCi [γ-³³P]ATP ，和 10 μl酶制剂。实验在室温下进行20分钟，最后加入10 μl 5 % H₃PO₄终止反应。沉淀物转移到GF/B 过滤器中，使用与96孔过滤器相配的万能采集器收集。通过闪烁计数器测定混合物的放射能。
细胞实验	细胞系	HUVEC, HUASMC,和BRP细胞系
	浓度	50 nM
	孵育时间	2小时
	方法	不同的肿瘤细胞系在96孔板上培养24小时。然后加入不同浓度的BIBF1120，处理72小时。通过Alamar-Blue染色的荧光强度测试EC50值。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	p-EGFR / FGFR1 / p-AKT / AKT / p-ERK / ERK Cyclin A / Cyclin D1 / Cyclin E / CDK2 / CDK4 / CDK6 p-SMAD3 / SMAD3 / p-p38 MAPK / p38 MAPK Fibronectin / Collagen 1a1		27581340
	Immunofluorescence	Vimentin / E-cadherin		29934570

体内研究(In Vivo)
体内研究活性	在小鼠的Fadu 移植瘤中，按鼠体重，每千克处理100mg BIBF1120,结果显示肿瘤血管密度降低76%。BIBF1120 作用于移植瘤模型Caki-1, HT-29, SKOV-3, Calu6 和PAC-120同样有显著的抑制效果。BIBF1120已用于治疗多种癌症，包括：非小细胞肺癌，前列腺癌，卵巢癌，及结肠直肠癌。且BIBF1120目前处于二期临床实验阶段。^[1]
动物实验	Animal Models	雌性无胸腺NMRI-nu/nu鼠
	Dosages	100 mg/kg
	Administration	口服处理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05676112	Withdrawn	Pulmonary Fibrosis	Boehringer Ingelheim\|China-Japan Friendship Hospital	December 29 2023	--
NCT06070610	Completed	Healthy	Boehringer Ingelheim	November 8 2023	Phase 1
NCT05755308	Not yet recruiting	Idiopathic Pulmonary Fibrosis	Fondazione Policlinico Universitario Agostino Gemelli IRCCS	October 2023	Not Applicable
NCT06071013	Not yet recruiting	Non-small Cell Lung Cancer\|EGFR Gene Mutation\|EGFR-TKI Resistant Mutation	China Medical University Hospital	September 28 2023	Phase 1\|Phase 2
NCT05817240	Completed	Idiopathic Pulmonary Fibrosis	Endeavor Biomedicines Inc.	May 3 2023	Phase 1

参考文献
[1] Hilberg F, et al. Cancer Res, 2008, 68(12), 4774-4782. [2] Frank H, et al. J Thorac Oncol, 2007, 2(8), S380. doi: 10.1097/01.JTO.0000283231.76336.01 [3] Roth GJ, et al. J Med Chem, 2009, 52(14), 4466-4480.

参考文献

化学信息&溶解度

分子量	539.62	分子式	C₃₁H₃₃N₅O₄
CAS号	656247-17-5	SDF	Download Nintedanib SDF
Smiles	CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)N=C(C3=CC=CC=C3)C4=C(NC5=C4C=CC(=C5)C(=O)OC)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 10 mg/mL ( (18.53 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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