Nintedanib esylate

Research use only, not for human use.

Nintedanib esylate (BIBF1120 esylate) is a potent triple angiokinase (VEGFR/PDGFR/FGFR) inhibitor.

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(In Vitro):Nintedanib (BIBF 1120) binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. Nintedanib (BIBF 1120) inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. Nintedanib (BIBF 1120) (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. Nintedanib (BIBF 1120) prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC).(In Vivo):Nintedanib (BIBF 1120) (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated.

Nintedanib (BIBF 1120) binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. Nintedanib (BIBF 1120) inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. Nintedanib (BIBF 1120) (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. Nintedanib (BIBF 1120) prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC).

Nintedanib (BIBF 1120) (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated.

BIBF1120 esylate | BIBF-1120 esylate

Angiogenesis

VEGFR

VEGFR1|VEGFR2|VEGFR3|FGFR1|FGFR2|FGFR3|PDGFRα|PDGFRβ

Cancer

Lung Cancer

656247-18-6

649.7571

C33H39N5O7S

>98% (HPLC)

10 mM in DMSO

CCS(=O)(=O)O.CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)N=C(C3=CC=CC=C3)C4=C(NC5=C4C=CC(=C5)C(=O)OC)O

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)

(-20℃)

With Ice Pack

≥ 2 years