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Nintedanib esylate

Catalog No. T5001 CAS 656247-18-6

Synonyms: Intedanib, BIBF 1120 (esylate), Nintedanib Ethanesulfonate Salt, BIBF 1120

Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Nintedanib esylate, CAS 656247-18-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 36.00
10 mg	In stock	$ 52.00
25 mg	In stock	$ 65.00
50 mg	In stock	$ 77.00
100 mg	In stock	$ 107.00
200 mg	In stock	$ 167.00
500 mg	In stock	$ 333.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 99.96%

Purity: 99.43%

Biological Description

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Description	Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β
Targets&IC50	PDGFRβ:65 nM, PDGFRα:59 nM, FGFR3:108 nM, FGFR1:69 nM, FGFR2:37 nM, VEGFR1:34 nM, VEGFR3:13 nM, VEGFR2:13 nM
In vitro	BIBF 1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC).
In vivo	BIBF1120, administered orally at doses ranging from 25-100 mg/kg daily, demonstrates high efficacy across various tumor models, including human tumor xenografts in nude mice and a syngeneic rat tumor model. Its effectiveness is confirmed through magnetic resonance imaging, which shows significant reductions in tumor perfusion, vessel density, and vessel integrity within 3 to 5 days, leading to substantial growth inhibition. Moreover, BIBF1120 is well-tolerated and exhibits promising results in in vivo tumor models, highlighting its potential as an effective oral therapeutic option.
Kinase Assay	Enzyme activity is assayed in the presence or absence of serial dilutions of BIBF1120 performed in 25% DMSO. Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound. All incubations are conducted at room temperature on a rotation shaker. 10 μL of each BIBF1120 dilution is added to 10 μL of diluted kinase (0.8 μg/mL VEGFR2, 10 mM Tris pH 7.5, 2 mM EDTA, and 2 mg/mL BSA) and preincubated for 1 hour. The reaction is started by addition of 30 μL of substrate mix containing 62.4 mM Tris pH 7.5, 2.7 mM DTT, 5.3 mM MnCl2, 13.3 mM Mg-acetate, 0.42 mM ATP, 0.83 mg/mL Poly-Glu-Tyr(4:1), and 1.7 μg/mL Poly-Glu-Tyr(4:1)-biotin and incubated for 1 hour. The reaction is stopped by addition of 50 μL of 250 mM EDTA, 20 mM HEPES, pH 7.4. 90 μL of the reaction mix is transferred to a streptavidin plate and incubated for 1-2 hours. After three washes with PBS the EU-labeled antibody, PY20 is added (recommended dilution 1:2000 of 0.5 mg/mL labeled antibody in DELFIA assay buffer). Excessive detection antibody is removed by three ishes of DELFIA washing buffer. Then 10 minutes before measurement on the multilabel reader, each well is incubated with 100 μL of DELFIA enhancement solution.
Animal Research	Five-week-old to 6-wk-old athymic NMRI-nu/nu female mice (21-31 g) are used for the assay. After acclimatization, mice are inoculated with 1 to 5×106 (in 100 μL) FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 cells s.c. into the right flank of the animal. After acclimatization, F344 Fischer rats are injected with 5×106 (in 100 μL) GS-9L cells s.c. into the right flank of the animal. For pharmacokinetic analysis, blood is isolated at indicated time points from the retroorbital plexus of mice and plasma is analyzed using high performance liquid chromatography-mass spectrometry methodology.

Synonyms	Intedanib, BIBF 1120 (esylate), Nintedanib Ethanesulfonate Salt, BIBF 1120
Molecular Weight	649.76
Formula	C31H33N5O4.C2H6O3S
CAS No.	656247-18-6

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 92.85 mg/mL (142.90 mM), Sonication and heating are recommended.

References and Literature

1. Roth GJ, 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, 52(14), 4466-4480. 2. Suzuki N, et al. Effect of a novel oral chemotherapeutic agent containing a combination of trifluridine, tipiracil and the novel triple angiokinase inhibitor nintedanib, on human colorectal cancer xenografts. Oncol Rep. 2016 Dec;36(6):3123-3130.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library FDA-Approved Kinase Inhibitor Library EMA Approved Drug Library Anti-Cancer Drug Library Inhibitor Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Nintedanib esylate 656247-18-6 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR PDGFR inhibit Platelet-derived growth factor receptor Nintedanib Intedanib BIBF1120 Fibroblast growth factor receptor BIBF-1120 BIBF 1120 (esylate) esylate Vascular endothelial growth factor receptor Inhibitor Nintedanib Ethanesulfonate Salt BIBF 1120 inhibitor

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