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Nintedanib

Description Mechanism of action indications Drugbank Description
Nintedanib
Nintedanib structure
CAS No.
656247-17-5
Chemical Name:
Nintedanib
Synonyms
100837;Nidanib;NTEDANIB;Vargatef;Intedanib;Nintedanib;Nintedanib-016;INTEDANIB BASE;Nintedanib whatsapp;Intedanib Vargatef
CBNumber:
CB72510401
Molecular Formula:
C31H33N5O4
Formula Weight:
539.62482
MOL File:
656247-17-5.mol

Nintedanib Properties

Boiling point:
742.2±60.0 °C(Predicted)
Density 
1.284±0.06 g/cm3(Predicted)
form 
Yellow solid.
pka
11.06±0.20(Predicted)
FDA UNII
G6HRD2P839

Nintedanib price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 11022 BIBF 1120 ≥95% 656247-17-5 10mg $35 2020-06-24 Buy
Cayman Chemical 11022 BIBF 1120 ≥95% 656247-17-5 50mg $88 2020-06-24 Buy
Cayman Chemical 11022 BIBF 1120 ≥95% 656247-17-5 100mg $158 2020-06-24 Buy
Cayman Chemical 11022 BIBF 1120 656247-17-5 250mg $350 2020-06-24 Buy

Nintedanib Chemical Properties,Uses,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.

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.

Nintedanib Preparation Products And Raw materials

Raw materials

Preparation Products


Nintedanib Suppliers

Global( 220)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Shenzhen Excellent Biotech Co., Ltd.
13480692018
ramyan@ex-biotech.com;sale@ex-biotech.com CHINA 959 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20039 58
Capot Chemical Co.,Ltd.
+86-571-85586718
+86-571-85864795 sales@capotchem.com China 19929 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21821 58
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
025-84209270 wgp@nanjing-pharmaceutical.com CHINA 115 55
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24723 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30045 58
Shenzhen Nexconn Pharmatechs Ltd
15013857715
admin@nexconn.com CHINA 3035 58

View Lastest Price from Nintedanib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2020-05-13 Nintedanib
656247-17-5
US $279.00 / mg 1g ≥98% 10kg BOC Sciences
2019-08-27 Nintedanib
656247-17-5
US $0.00-0.00 / KG 1g 99.0% 200kg/month Beijing Yibai Biotechnology Co., Ltd
2018-08-21 Nintedanib
656247-17-5
US $7.00 / KG 1KG 99% 1000KG career henan chemical co

656247-17-5(Nintedanib)Related Search:


  • Nidanib
  • NINTEDANIB; BIBF1120; VARGATEF; BIBF-1120
  • Nintedanib-016
  • Nintedanib (Intedanib)
  • methyl (3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylate Nintedanib (BIBF 1120)
  • Vargatef (nintedanib)
  • 3-[(4-{Methyl-[2-(4-methyl-piperazin-1-yl)-acetyl]-amino}-phenylamino)-phenyl-methylene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester
  • 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone
  • Nintedanib, Free Base, >99%
  • methyl (3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylate
  • NTEDANIB
  • methyl (3Z)-2-hydroxy-3-[({4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-3H-indole-6-carboxylate
  • (3Z)-2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-Indole-6-carboxylic acid methyl ester
  • methyl (Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylate
  • Methyl (Z)-3-[[[4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl]amino](phenyl)methylene]-2-oxoindoline-6-carboxylate
  • BIBF-1120(Nintedanib,Vargatef)
  • Intedanib
  • BIBF 1120; VARGATEF; INTEDANIB
  • Vargatef
  • Nintedanib whatsapp
  • Intedanib (Nintedanib)
  • 1H-Indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester, (3Z)-
  • (3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylate
  • methyl (3Z)-3-{[(4-{methyl[(4-methylpiperazin-1-yl)acetyl]amino}phenyl)amino](phenyl)methylidene
  • Vargatef (BIBF 1120, Intedanib)
  • BIBF1120;VARGATEF;BIBF-1120
  • INTEDANIB BASE
  • Nintedanib
  • Nintedanib (BIBF 1120)
  • Nintedanib/Intedanib/Vargatef
  • BIBF 1120; VARGATEF; INTEDANIB;INTEDANIB BASE
  • Intedanib Vargatef
  • 100837
  • 656247-17-5
  • C31H33O4N5
  • API
  • Inhibitors
  • Amines
  • Nintedanib
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
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