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Nintedanib esylate

CAT: 0013-GTR19161092-01Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19161092-01Size:1 g
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Description
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.
CAS Number
656247-18-6
Product Name Alternative
BIBF1120 esylate | BIBF-1120 esylate
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
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
Molecular Formula
C33H39N5O7S
Molecular Weight
649.7571
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
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)

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T5001-01Nintedanib esylate
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A16197-10Nintedanib esylate 10mg
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A16197-50Nintedanib esylate 50mg

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