Search Site
Home >> Signaling Pathways >> Tyrosine Kinase/Adaptors >> PDGFR >> Nintedanib (BIBF 1120)
Related Biochemicals Related Antibodies

Nintedanib (BIBF 1120)

Multi-target kinase inhibitor, inhibits VEGFR, PDGFR, and FGFR

Nintedanib (BIBF 1120)

Catalog No. A8252
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
5mg $90.00 In stock
25mg $177.00 In stock

All inclusive: Shipping and all other fees included

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Nintedanib(BIBF 1120)

Related Biological Data

Nintedanib(BIBF 1120)

Related Biological Data

Nintedanib(BIBF 1120)

Biological Activity

Description Nintedanib (BIBF 1120) is a potent inhibitor of triple angiokinase for 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.
Targets VEGFR1/2/3 FGFR1/2/3 PDGFRα/β      
IC50 34 nM/13 nM/13 nM 69 nM/37 nM/108 nM 59 nM/65 nM      

Nintedanib (BIBF 1120) Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Nintedanib (BIBF 1120) Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 928326-83-4 SDF Download SDF
Synonyms Vargatef
Chemical Name methyl (3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylate
Canonical SMILES CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)NC(=C3C4=C(C=C(C=C4)C(=O)OC)NC3=O)C5=CC=CC=C5
Formula C31H33N5O4 M.Wt 539.62
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

View Related Products By Research Topics

Background

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 trials, including non-small cell lung cancer8, ovarian cancer6, colorectal cancer7, hepatocellular carcinoma9 and many other solid tumors. In addition, the possibilities of combining Nintedanib therapy with other treatments such as docetaxel10 and afatinib 11are being tested in different tumor models. The most common drug-related adverse events in patients were diarrhea, nausea, vomiting and lethargy7.

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).[2]Roth, G. J. 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). Journal of medicinal chemistry 52, 4466-4480, doi:10.1021/jm900431g (2009).[3]Wollin, L., Maillet, I., Quesniaux, V., Holweg, A. & Ryffel, B. Antifibrotic and Anti-inflammatory Activity of the Tyrosine Kinase Inhibitor Nintedanib in Experimental Models of Lung Fibrosis. The Journal of pharmacology and experimental therapeutics 349, 209-220, doi:10.1124/jpet.113.208223 (2014).[4]Antoniu, S. A. Nintedanib (BIBF 1120) for IPF: a tomorrow therapy? Multidisciplinary respiratory medicine 7, 41, doi:10.1186/2049-6958-7-41 (2012).[5]Santos, E. S., Gomez, J. E. & Raez, L. E. Targeting angiogenesis from multiple pathways simultaneously: BIBF 1120, an investigational novel triple angiokinase inhibitor. Investigational new drugs 30, 1261-1269, doi:10.1007/s10637-011-9644-2 (2012).[6]Wei, X. W., Zhang, Z. R. & Wei, Y. Q. Anti-angiogenic drugs currently in Phase II clinical trials for gynecological cancer treatment. Expert opinion on investigational drugs 22, 1181-1192, doi:10.1517/13543784.2013.812071 (2013).[7]Mross, K. et al. Phase I study of the angiogenesis inhibitor BIBF 1120 in patients with advanced solid tumors. Clinical cancer research : an official journal of the American Association for Cancer Research 16, 311-319, doi:10.1158/1078-0432.CCR-09-0694 (2010).[8]Rolfo, C. et al. BIBF 1120/ nintedanib : a new triple angiokinase inhibitor-directed therapy in patients with non-small cell lung cancer. Expert opinion on investigational drugs 22, 1081-1088, doi:10.1517/13543784.2013.812630 (2013).[9]Tai, W. T. et al. Nintedanib (BIBF-1120) inhibits hepatocellular carcinoma growth independent of angiokinase activity. Journal of hepatology, doi:10.1016/j.jhep.2014.03.017 (2014).[10]Reck, M. et al. Docetaxel plus nintedanib versus docetaxel plus placebo in patients with previously treated non-small-cell lung cancer (LUME-Lung 1): a phase 3, double-blind, randomised controlled trial. The lancet oncology 15, 143-155, doi:10.1016/S1470-2045(13)70586-2 (2014).[11]Bouche, O. et al. Phase II trial of weekly alternating sequential BIBF 1120 and afatinib for advanced colorectal cancer. Anticancer research 31, 2271-2281 (2011).