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Nintedanib (BIBF 1120)

Product #: TS0168
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l  General Information

Product Name

Nintedanib (BIBF 1120)

General description

Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase  3.

Synonym

methyl  (3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6 carboxylate; Intedanib

Purity

98.0%(HPLC)

CAS Number

656247-17-5

Formula

C31H33N5O4

Molecular Weight

539.62

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

solid

Solubility(25℃)

DMSO

≥5mg/mL

Ethanol

~3mg/mL

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Nintedanib is an orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor with potential  antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase  inhibitor BIBF 1120 selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. In addition, this agent also inhibits members of the Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3 (fms-like tyrosine kinase 3). VEGFR, FGFR and PDGFR RTKs play key roles in tumor angiogenesis.

Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays.

Application

1. Antineoplastic Agents

2. Enzyme Inhibitors

3. Nintedanib is an orally available tyrosine kinase receptor antagonist that inhibits collagen formation and is used to treat idiopathic pulmonary fibrosis.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov

 

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