Nintedanib esylate

SKU: orb1302268

Description

Nintedanib esylate (BIBF 1120 esylate) is a small molecule triple kinase inhibitor targeting VEGFR, FGFR, and PDGFR receptors. It is widely used in preclinical research to study angiogenesis, fibrosis, and oncology in both cellular assays and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 656247-18-6
• MW: 649.76
• Purity: 99.98%
• Formula: C₃₁H₃₃N₅O₄.C₂H₆O₃S
• SMILES: CCS(O)(=O)=O.COC(=O)c1ccc2c(NC(=O)\C2=C(/Nc2ccc(cc2)N(C)C(=O)CN2CCN(C)CC2)c2ccccc2)c1
• Target: VEGFR,PDGFR,FGFR
• Solubility: DMSO:101 mg/mL (155.44 mM)

Bioactivity

• Target IC50:
  VEGFR3:13 nM|VEGFR1:34 nM|FGFR2:37 nM|VEGFR2:13 nM|FGFR3:108 nM|PDGFRβ:65 nM|PDGFRα:59 nM|FGFR1:69 nM
• 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.
• 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).
• 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.

Storage & Handling

• Storage: keep away from direct sunlight,keep away from moisture,store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Nintedanib, Nintedanib esylate, Nintedanib Ethanesulfonate Salt, PDGFRβ, PDGFRα, PDGFR, FGFR, FGFR1, FGFR2, FGFR3, esylate, BIBF 1120 (esylate), BIBF1120, BIBF-1120, VEGFR3, VEGFR2, VEGFR1, VEGFR

Compound Identifiers

PubChem CID

135476717