Nintedanib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的三重血管激酶 (VEGFR/PDGFR/FGFR) 抑制剂，对 VEGFR-2/FGFR-1/PDGFRα/VEGFR-1/VEGFR-3 的 IC50 分别为 5/38/18/104/5 nM。

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.

BIBF-1120 | BIBF1120

Angiogenesis

VEGFR

FLT3|Lck|VEGFR1|VEGFR2|VEGFR3|FGFR1|FGFR2|PDGFRα

Cancer

Lung Cancer

656247-17-5

539.6248

C31H33N5O4

>98% (HPLC)

10 mM in DMSO

CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)N/C(=C\3/C4=C(C=C(C=C4)C(=O)OC)NC3=O)/C5=CC=CC=C5

(Z)-methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate

(-20℃)

With Ice Pack

≥ 2 years