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Nintedanib esylate

Chemical Structure : Nintedanib esylate

CAS No.: 656247-18-6

Nintedanib esylate (BIBF1120 esylate;BIBF-1120 esylate)

Catalog No.: PC-42813Not For Human Use, Lab Use Only.

Nintedanib esylate (BIBF1120 esylate) is a potent triple angiokinase (VEGFR/PDGFR/FGFR) inhibitor with IC50 of 5/38/18/104/5 nM for VEGFR-2/FGFR-1/PDGFRα/VEGFR-1/VEGFR-3, respectively.

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Biological Activity

Nintedanib esylate (BIBF1120 esylate) is a potent triple angiokinase (VEGFR/PDGFR/FGFR) inhibitor with IC50 of 5/38/18/104/5 nM for VEGFR-2/FGFR-1/PDGFRα/VEGFR-1/VEGFR-3, respectively; inhibits MAPK and Akt signaling pathways, show inhibition of cell proliferation (EC50=10-80 nM); is fully efficacious in xenograft models and orally active.

Lung Cancer

Approved

Physicochemical Properties

M.Wt 649.7571
Formula C33H39N5O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester, (3Z)-, ethanesulfonate (1:1)

References

1. Roth GJ, et al. J Med Chem. 2009 Jul 23;52(14):4466-80.

2. Hilberg F, et al. Cancer Res. 2008 Jun 15;68(12):4774-82.

3. Kudo K, et al. Clin Cancer Res. 2011 Mar 15;17(6):1373-81.

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