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Nintedanib (BIBF 1120)

Cat. No. M5331
Nintedanib (BIBF 1120) Structure
Synonym:

Intedanib

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 290 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 539.62
Formula C31H33N5O4
CAS Number 656247-17-5
Purity >99%
Solubility 6 mg/mL in DMSO
Storage at -20°C
References

What could Nintedanib (BIBF 1120), a triple inhibitor of VEGFR, PDGFR, and FGFR, add to the current treatment options for patients with metastatic colorectal cancer?
Capdevila J, et al. Crit Rev Oncol Hematol. 2014 Nov;92(2):83-106. PMID: 24924525.

Nintedanib (BIBF-1120) inhibits hepatocellular carcinoma growth independent of angiokinase activity.
Tai WT, et al. J Hepatol. 2014 Jul;61(1):89-97. PMID: 24657398.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Nintedanib (BIBF 1120), Intedanib supplier, VEGFR/PDGFR, inhibitors

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