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Nintedanib/尼达尼布 {[allProObj[0].p_purity_real_show]}

货号：A181556 同义名： BIBF 1120; Intedanib

Nintedanib（BIBF 1120）是一种强效的三重血管激酶抑制剂，对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、59 nM和65 nM。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Nintedanib/尼达尼布 化学结构 CAS号：656247-17-5
Nintedanib/尼达尼布 化学结构
CAS号：656247-17-5
Nintedanib/尼达尼布 3D分子结构
CAS号：656247-17-5
Nintedanib/尼达尼布 化学结构 CAS号：656247-17-5
Nintedanib/尼达尼布 3D分子结构 CAS号：656247-17-5
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Nintedanib/尼达尼布 纯度/质量文件 产品仅供科研

货号：A181556 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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Nintedanib/尼达尼布 生物活性

靶点

  • VEGFR1

    VEGFR1, IC50:34 nM

  • VEGFR3

    VEGFR3, IC50:13 nM

  • VEGFR2

    VEGFR2, IC50:13 nM

  • PDGFRβ

    PDGFRβ, IC50:65 nM
描述 VEGF/VEGFR (vascular endothelial growth factor/vascular endothelial growth factor receptor) pathway plays a key role in tumor angiogenesis by promotion of vascular and lymphatic endothelial, as well as survival, and invasion, thus resulting in neovascularization, tumor growth and metastasis. In addition, blockade of additional proangiogenic receptor tyrosine kinases, including PDGFR and FGFR, may improve long-term clinical outcomes. BIBF 1120 is a multi-RTKs inhibitor with IC50 values of 13nM, 13nM , 16nM , 26nM , 34nM , 37nM , 59nM , 65nM , 69nM , 108nM for VEGFR2, VEGFR3, LCK, FLT3, VEGFR1, FGFR2, PDGFRα, PDGFRβ, FGFR1, FGFR3 (measured by enzymatic assays), less potent to Src, Lyn and FGFR4 with IC50 values of 156nM , 195nM and 610nM, respectively. Treatment with BIBF 1120 resulted in cell proliferation and apoptosis (EC50<10nM) in HUVECs, HSMECs, as well as the downstream p-MAPK and p-AKT (0.1-1μM). Daily oral treatment with BIBF 1120 at dose of 100mg/kg for 5 days reduced vessel density by 76% in FaDu xenografts, as well as markedly reduced both Meca 32–positive and PDGFRβ-positive cells predominantly in the intratumoral compartment. Once daily oral administration of BIBF 1120 at dose of 50mg/kg and 100mg/kg inhibited tumor growth both in a model of human head and neck small cell carcinoma (FaDu cells) and in a human renal cancer model (Caki-1 cells)[1].
作用机制 BIBF 1120 is ATP-competitive proangiogenic receptor tyrosine kinase inhibitor, which can bound in the active site of the VEGFR-2.[1]

Nintedanib/尼达尼布 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
A549 2/5 μM Function Assay 24 h has a general EMT reversal effect  26061747
A549 0.01–5 μM Function Assay 24 h induces SFTPD mRNA expression dose dependently 25843005
A549 0.01–5 μM Function Assay 72 h enhances SP-D protein expression in a dose-dependent manner at concentrations of up to 5 μM  25843005
A549 5 μM Function Assay 0-1 h increases AP-1 activation after 30 min 25843005

Nintedanib/尼达尼布 动物研究

Dose Mice: 50 mg/kg[2] (p.o.), 3 mg/kg - 100 mg/kg[3] (p.o.); 5 mg/kg[4] (i.p.)
Rat: 25 mg/kg - 100 mg/kg[1] (p.o.)
Administration p.o., i.p.
Pharmacokinetics
Animal Mice[5] Rats[5] Monkeys[5]
Dose 50 mg/kg 50 mg/kg (p.o.)
2 mg/kg (i.v.) 		40 mg/kg (p.o., cynomolgus monkey)
5 mg/kg (i.v., cynomolgus monkey)
Administration p.o. p.o.
i.v. 		p.o.
i.v.
MRT 5.19 h 3.25 h (i.v.) 3.82 h (i.v.)
F 11.9% (p.o.) 13.2% (p.o.)
T1/2 5.15 h 3.95 h (i.v.) 5.95 h (i.v.)
AUC 2720 ng·h/ml 375 ng·h/ml (p.o.)
181 ng·h/ml (i.v.) 		2390 ng·h/ml (p.o.)
2260 ng·h/ml (i.v.)
CL 202 ml/min/kg (i.v.) 37.5 ml/min/kg (i.v.)
Cmax 547 ng/ml 105 ng/ml (p.o.)
124 ng/ml (i.v.) 		175 ng/ml (p.o.)
1300 ng/ml (i.v.)
Protein bound (%) 92.9% (p.o.)
Protein binding (free drug %) 0.972 98.5% (p.o.)
Vss 41.2 L/kg (i.v.) 8.64 L/kg (i.v.)

Nintedanib/尼达尼布 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03361319 NSCLC, Recurrent ... 展开 >> Adenocarcinoma of Lung 收起 << Phase 1 Phase 2 Not yet recruiting January 2022 -
NCT02863055 Malignant Pleural Mesothelioma Phase 2 Recruiting October 2020 Belgium ... 展开 >> UZ Antwerpen Recruiting Antwerpen, Belgium Contact: Jan Van Meerbeeck, prof          UZ Gent Recruiting Gent, Belgium Contact: Veerle Surmont, Prof          Italy Ospedale San Paolo Recruiting Milan, Italy Contact: Andrea Luciani, Dr          United Kingdom Manchester University NHS Foundation Trust - UHSM-Wythenshawe Hospital Recruiting Wythenshawe, Manchester, United Kingdom, M23 9LT Principal Investigator: Paul Taylor          Royal Marsden Hospital Recruiting Chelsea, United Kingdom Contact: Sanjay Popat, Dr          Royal Marsden Hospital - Kingston Recruiting Kingston, United Kingdom Contact: Sanjay Popat, Dr          Sheffield Teaching Hospitals NHS Foundation Trust - Weston Park Hospital Recruiting Sheffield, United Kingdom Contact: Robin Young, Dr          NHS South Tyneside-South Tyneside District Hospital Recruiting South Shields, United Kingdom Contact: Rhona McMenemin, Dr          Royal Marsden Hospital Recruiting Sutton, United Kingdom Contact: Sanjay Popat, Dr 收起 <<
NCT02597933 Scleroderma, Systemic Phase 3 Completed - -

Nintedanib/尼达尼布 参考文献

[1]Hilberg F, Roth GJ, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82.

[2]Roth GJ, Heckel A, 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 Jul 23;52(14):4466-80.

[3]Wollin L, Maillet I, et al. Antifibrotic and anti-inflammatory activity of the tyrosine kinase inhibitor nintedanib in experimental models of lung fibrosis. J Pharmacol Exp Ther. 2014 May;349(2):209-20.

[4]Öztürk Akcora B, Storm G, et al. Tyrosine kinase inhibitor BIBF1120 ameliorates inflammation, angiogenesis and fibrosis in CCl4-induced liver fibrogenesis mouse model. Sci Rep. 2017 Mar 14;7:44545.

[5]Nintedanib

Nintedanib/尼达尼布 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.19mL

9.27mL

1.85mL

0.93mL

18.53mL

3.71mL

1.85mL

Nintedanib/尼达尼布 技术信息

CAS号656247-17-5
分子式C31H33N5O4
分子量 539.62
SMILES Code O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(N(C)C(CN4CCN(C)CC4)=O)C=C3)/C5=CC=CC=C5)OC
MDL No. MFCD11974012
别名 BIBF 1120; Intedanib
运输蓝冰
InChI Key CPMDPSXJELVGJG-UHFFFAOYSA-N
Pubchem ID 135423438
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

DMSO: 10 mg/mL(18.53 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在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
方案 二

Tags: Nintedanib | BIBF 1120;Intedanib | VEGFR | PDGFR | FGFR | AmBeed-信号通路专用抑制剂 | Nintedanib/尼达尼布 纯度/质量文件 | Nintedanib/尼达尼布 生物活性 | Nintedanib/尼达尼布 细胞研究 | Nintedanib/尼达尼布 动物研究 | Nintedanib/尼达尼布 临床数据 | Nintedanib/尼达尼布 参考文献 | Nintedanib/尼达尼布 实验方案 | Nintedanib/尼达尼布 技术信息

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