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PDGFR&FGFR

Nintedanib (BIBF 1120) (656247-17-5)

Nintedanib(BIBF 1120) is 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.

Not Intended for Therapeutic Use. For research use only.

CAS: 656247-17-5 Category

Nintedanib (BIBF 1120) (656247-17-5) Description:

Nintedanib(BIBF 1120) is an orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhibitor BIBF 1120 selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. In addition, this agent also inhibits members of the Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3 (fms-like tyrosine kinase 3). VEGFR, FGFR and PDGFR RTKs play key roles in tumor angiogenesis.

Nintedanib(BIBF1120) inhibits PDGFR kinase activity of PDGFR alpha and PDGFR beta types with IC50 values of 59 nM and 65 nM, respectively. In addition, BIBF1120 suppresses the FGFR subtypes with IC50 of 60 nM, 37 nM and 108 nM for FGFR1, FGFR2, and FGFR3, respectively. BIBF1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. The indolinone scaffold forms two hydrogen bonds with the backbone nitrogen of Cys919 and the backbone carbonyl oxygen of Glu917 in the hinge region. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 at concentrations as low as 100 nM blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. In cultures of human vascular smooth muscle cells (HUASMC), BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM.

Nintedanib (BIBF 1120) (656247-17-5) Specifications:

Product Name Nintedanib (BIBF 1120)
Synonym BIBF1120; BIBF 1120; BIBF-1120; Nintedanib. Brand name: Vargatef.
Chemical Name (Z)-methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate
Purity ≥98% (HPLC)
CAS Number 656247-17-5
Molecular Formula C31H33N5O4
Molecular Weight 539.636 g/mol
Monoisotopic Mass 539.253 g/mol
MDL number MFCD03095196
InChIKey XZXHXSATPCNXJR-ZIADKAODSA-N
InChi Code InChI=1S/C31H33N5O4/c1-34-15-17-36(18-16-34)20-27(37)35(2)24-12-10-23(11-13-24)32-29(21-7-5-4-6-8-21)28-25-14-9-22(31(39)40-3)19-26(25)33-30(28)38/h4-14,19,32H,15-18,20H2,1-3H3,(H,33,38)/b29-28-
SMILES 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
Form Powder
Color yellow
Solubility  DMSO 17 mg/mL (31.50 mM)

Water Insoluble

Alcohol 4 mg/mL (7.41 mM)

Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application a kinase inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Lung function outcomes in the INPULSIS® trials of nintedanib in idiopathic pulmonary fibrosis. Brown KK, Flaherty KR, Cottin V, Raghu G, Inoue Y, Azuma A, Huggins JT, Richeldi L, Stowasser S, Stansen W, Schlenker-Herceg R, Maher TM, Wells AU. Respir Med. 2019 Jan;146:42-48. doi: 10.1016/j.rmed.2018.11.012. Epub 2018 Nov 19. PMID: 30665517

[2]. Nintedanib inhibits TGF-β-induced myofibroblast transdifferentiation in human Tenon’s fibroblasts. Lin X, Wen J, Liu R, Gao W, Qu B, Yu M. Mol Vis. 2018 Dec 9;24:789-800. eCollection 2018. PMID: 30636861

[3]. Effect of nintedanib on airway inflammation in a mouse model of acute asthma. Lee J, Rhee CK, Lee JH, Yoon HJ, Kim IK, Hur J, Kang JY, Yoon HK, Lee SY, Kim YK. J Asthma. 2019 Jan 11:1-10. doi: 10.1080/02770903.2018.1544641. [Epub ahead of print] PMID: 30634874

[4]. Raghu G, Wells AU, Nicholson AG, Richeldi L, Flaherty KR, Le Maulf F, Stowasser S, Schlenker-Herceg R, Hansell DM. Effect of Nintedanib in Subgroups of Idiopathic Pulmonary Fibrosis by Diagnostic Criteria. Am J Respir Crit Care Med. 2016 Jun 22. [Epub ahead of print] PubMed PMID: 27331880.

[5]. Nintedanib. Aust Prescr. 2016 Apr;39(2):62-3. doi: 10.18773/austprescr.2016.031. Epub 2016 Feb 22. Review. PubMed PMID: 27340326; PubMed Central PMCID: PMC4917623.

1 review for Nintedanib (BIBF 1120) (656247-17-5)

  1. Cofttek

    Never had such good experience before,The Nintedanib (BIBF 1120) (656247-17-5) is high purity,also customer service is pretty nice !gotta try!!

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