Nintedanib esylate

SKU: orb1302268

Description

Nintedanib esylate

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: FGFR,VEGFR,PDGFR
• 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 betwee the amino and carboxy terminal lobes o 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 musclee cells (HUASMC).
• Animal Research:
  Five-week-old to 6-wk-old athymic nMRI-nu/nu f Male mice (21-31 g) are used fo the assay. After acclimatization, mice are inoculated with 1 to × 06 (in 100 μL) FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 cells s.c. int the right flank o the animal. After acclimatization, F344 Fischer rats are injected with × 06 (in 100 μL) GS-9L cells s.c. int the right flank o the animal. For pharmacokinetic analysis, blood is isolated at indicated time points fro 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.
• 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