Description Mechanism of action indications Drugbank Description
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Nintedanib

Description Mechanism of action indications Drugbank Description
Product Name
Nintedanib
CAS No.
656247-17-5
Chemical Name
Nintedanib
Synonyms
Intedanib;Nintedanib (BIBF 1120);INTEDANIB BASE;methyl (3Z)-3-{[(4-{methyl[(4-methylpiperazin-1-yl)acetyl]amino}phenyl)amino](phenyl)methylidene;(3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylate;methyl (3Z)-2-hydroxy-3-[({4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-3H-indole-6-carboxylate;100837;Nidanib;NTEDANIB;Vargatef
CBNumber
CB72510401
Molecular Formula
C31H33N5O4
Formula Weight
539.64
MOL File
656247-17-5.mol
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Nintedanib Property

Melting point:
>237oC (dec.)
Boiling point:
742.2±60.0 °C(Predicted)
Density 
1.284±0.06 g/cm3(Predicted)
storage temp. 
Refrigerator
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
Yellow solid.
pka
11.06±0.20(Predicted)
color 
Light Yellow to Light Green
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Safety

Hazardous Substances Data
656247-17-5(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
11022
Product name
BIBF 1120
Purity
≥95%
Packaging
10mg
Price
$39
Updated
2023/01/06
Cayman Chemical
Product number
11022
Product name
BIBF 1120
Purity
≥95%
Packaging
50mg
Price
$96
Updated
2023/01/06
Cayman Chemical
Product number
11022
Product name
BIBF 1120
Purity
≥95%
Packaging
100mg
Price
$171
Updated
2023/01/06
Cayman Chemical
Product number
11022
Product name
BIBF 1120
Packaging
250mg
Price
$379
Updated
2023/01/06
Tocris
Product number
7049
Product name
Nintedanib
Purity
≥98%(HPLC)
Packaging
10
Price
$59
Updated
2021/12/16
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Nintedanib Chemical Properties,Usage,Production

Description

Nintedanib is an oral administrated triple tyrosine kinase inhibitors developed by Boehringer Ingelheim, Germany. Its targets include platelet-derived growth factor (PDGF), vascular endothelial growth factor (VEGF) and basic fiber (BFGF), being able to also inhibit the activation of MAPK and Akt. At present, it is mainly used for cancer treatment, such as colorectal cancer, ovarian cancer and multiple myeloma. The study regarding to the respiratory diseases mainly focuses on the clinical treatment of advanced non-small cell lung cancer (NSCLC) and idiopathic pulmonary fibrosis (IPF). In June 2014, Boehringer Ingelheim has announced that the marketing authorization application of Nintedanib for the treatment of Idiopathic Pulmonary Fibrosis (IPF) had been confirmed by the European Medicines Agency (EMA) and been included in the accelerated approval list by the EMA.

Mechanism of action

Nintedanib is a small molecule that targets multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Among them, FGFR, PDGFR, and VEGFR have been implicated in IPF pathogenesis. Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts representing essential mechanisms of the IPF pathology. In addition, nintedanib inhibits the following nRTKs: Lck, Lyn and Src kinases. The contribution of FLT3 and nRTK inhibition to IPF efficacy is unknown.

indications

Nintedanib ( Vargatef ) is an oral triple angiokinase inhibitor which simultaneously inhibits vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR) and fibroblast growth factor receptors (FGFR) signalling pathways. Growing scientific evidence shows that these three different angiokinase receptors play an important role not only in angiogenesis but also in tumour growth and metastasis.
Nintedanib is currently being investigated in patients with various solid tumours including Phase III studies in advanced NSCLC, colorectal cancer (refractory to standard treatment) and ovarian cancer, and also in Phase II studies in mesothelioma, kidney cancer (renal cell carcinoma) and liver cancer (hepatic cell carcinoma).
In the EU, nintedanib in the treatment of idiopathic pulmonary fibrosis (IPF) has recently received a positive CHMP opinion. The U.S. Food and Drug Administration (FDA) has approved nintedanib capsules under the brand name OFEV for oral use for the treatment of IPF.

Drugbank Description

Nintedanib is a drug indicated for the treatment of idiopathic pulmonary fibrosis (IPF) that targets multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Among them, FGFR, PDGFR, and VEGFR have been implicated in IPF pathogenesis. Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts representing essential mechanisms of the IPF pathology. In addition, nintedanib inhibits the following nRTKs: Lck, Lyn and Src kinases. The contribution of FLT3 and nRTK inhibition to IPF efficacy is unknown. Idiopathic pulmonary fibrosis (IPF) is a progressive and ultimately fatal lung disease characterized by a progressive loss of lung function with worsening dyspnoea and cough. Development is thought to be instigated by repetitive lung injury (such as by cigarette smoke, industrial dusts, gastrooesophageal reflux and viral infection) leading to destruction of epithelial alveolar cells. Subsequent dysregulation of the repair process results in the proliferation/migration of fibroblasts and their differentiation into myofibroblasts, abnormal extracellular matrix deposition and excessive collagen accumulation in the lung interstitium and alveolar space, leading to progressive fibrosis and stiffening of the lungs. Vascular endothelial growth factor (VEGF), fibroblast growth factor (FGF) and platelet-derived growth factor (PDGF) mediate various processes, including fibrogenesis and angiogenesis, and are implicated in the pathogenesis of IPF. By blocking substrate binding and downstream signalling cascades, nintedanib interferes with processes active in fibrosis such as fibroblast proliferation, migration and differentiation, and the secretion of extracellular matrix.
References
https://www.drugbank.ca/drugs/DB09079

Uses

It is an indolinone derivative potently blocking VEGF-, PDGF-, and FGF-receptor kinases; an indolinone as triple angiokinase inhibitors.

Uses

BIBF1120 (Vargatef) is a potent inhibitor of VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

Uses

It is an indolinone derivative potently blocking VEGF-, PDGF-, and FGF-receptor kinases; an indolinone as triple angiokinase inhibitors. An antitumor agent.

Definition

ChEBI: A member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer.

Biological Activity

nintedanib (bibf 1120) is an indolinone-derived oral active, triple angiokinase inhibitor of vascular endothelial growth factor receptor (vegfr)1-3, fibroblast growth factor receptor (fgfr)1-3 and platelet-derived growth factor receptor (pdgfr)α/β1. it has shown potent antiangiogenic activity at nanomolar (ic50, 20-100 nmol/l) by blocking these receptor-mediated signaling pathways1,2. nintedanib (bibf 1120) is in clinical development for the treatment of idiopathic pulmonary fibrosis as these receptors have been shown to be potentially involved in the pathogenesis of pulmonary fibrosis3,4. as a novel angiogenesis inhibitor, it is also being widely evaluated in different cancer models and has displayed significant anti-tumor activities by inhibiting tumor blood vessel formation5-7.to further evaluate its antitumor effects on multiple tumors, nintedanib is currently entering several

Clinical Use

Tyrosine kinase inhibitor:
Treatment of locally advanced, metastatic or locally recurrent non-small cell lung cancer (NSCLC) of adenocarcinoma tumour histology in combination with docetaxel
Treatment of Idiopathic Pulmonary Fibrosis (IPF)

Drug interactions

Potentially hazardous interactions with other drugs
Antibacterials: concentration reduced by rifampicin - avoid.
Antifungals: concentration increased by ketoconazole.
Antipsychotics: increased risk of agranulocytosis with clozapine - avoid.

Metabolism

Nintedanib is metabolised in the liver, initially by hydrolytic cleavage by esterases and then by glucuronidation by uridine diphosphate glucuronosyltransferase enzymes. Only a minor portion is metabolised by cytochrome P450 isoenzymes, mainly CYP3A4. More than 90% of a dose is eliminated by faecal/biliary excretion.

References

[1]hilberg, f. et al. bibf 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. cancer research 68, 4774-4782, doi:10.1158/0008-5472.can-07-6307 (2008).

Nintedanib Preparation Products And Raw materials

Raw materials

Preparation Products

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Nintedanib Suppliers

Jinan XuanDe Chemical Co., Ltd.
Tel
0531-88803958 18866891188
Fax
0531-82777287
Email
xuandechem@126.com
Country
China
ProdList
224
Advantage
58
Shandong Haiwo Biological Technology Co., Ltd.
Tel
0531-87586188 13046003282
Fax
0531-87586188
Email
sales@hwbiology.com
Country
China
ProdList
50
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58
Giant chemicals
Tel
028-85434334 18108076537
Fax
QQ:245797092
Email
market@gianthx.com
Country
China
ProdList
4512
Advantage
56
Nanjing Puxin Pharmaceutical Technology Co., Ltd
Tel
17366295326
Fax
QQ360829978
Email
puxinpharma_2017@126.com
Country
China
ProdList
2525
Advantage
58
Shanghai Jinyin Biological Technology Co., Ltd
Tel
18019349802
Email
814527417@qq.com
Country
China
ProdList
365
Advantage
58
Shandong Yuhe Pharmaceutical Technology Co., LTD
Tel
15263077727 15263077727
Fax
QQ:2938966534
Email
1436425847@qq.com
Country
China
ProdList
177
Advantage
58
Cangzhou Kangrui Medical Technology Co., LTD
Tel
18632776803
Email
355803330@qq.com
Country
China
ProdList
416
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2923
Advantage
55
Hangzhou Zyter Biological & Chemical Technology Co., Ltd.
Tel
18858184290
Fax
0086-571-28313105
Email
sales@zyterpharm.com
Country
China
ProdList
48
Advantage
49
Chembest Research Laboratories Limited
Tel
021-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6002
Advantage
61
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View Lastest Price from Nintedanib manufacturers

HangZhou RunYan Pharma Technology Co.,LTD.
Product
Nintedanib 656247-17-5
Price
US $0.00/kg
Min. Order
1kg
Purity
99% HPLC
Supply Ability
1000kg
Release date
2022-11-07
Wuhan Biocar Pharmacy Co., Ltd.
Product
Nintedanib 656247-17-5
Price
US $9.90-1277.00/g
Min. Order
10g
Purity
99.99%HPLC.USP42——Powder、Oil、Pills、Capsules、Tablets,Customized packaging
Supply Ability
100KG/Month
Release date
2022-10-21
Henan Aochuang Chemical Co.,Ltd.
Product
Nintedanib 656247-17-5
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1Ton
Release date
2022-09-22

656247-17-5, NintedanibRelated Search:


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