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Nintedanib
- BIBF-1120
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C31H33N5O4
- MW: 539.62
Description
Nintedanib (BIBF-1120) is an oral small-molecule receptor tyrosine kinase (RTK) inhibitor exhibiting powerful antifibrotic and antiangiogenic properties. It competitively blocks VEGFR1-3 (IC50: 34 nM, 21 nM, and 13 nM), PDGFRα and β (IC50: 59 and 65 nM), and FGFR1-3 (IC50: 69 nM, 37 nM, and 108 nM). In addition, it also inhibits Src family kinases, including Src, Lck, Lyn, and FLT-3 (IC50: 156 nM, 16 nM, 195 nM, and 26 nM). Nintedanib disrupts downstream signaling cascades crucial for cellular proliferation. Consequently, it suppresses lung fibroblast activation, inhibits myofibroblast differentiation, and significantly slows disease progression in idiopathic pulmonary fibrosis.
RTK pharmacology is highly relevant to tumor pathogenesis and angiogenesis. As a multi-targeted angiokinase inhibitor, Nintedanib (BIBF-1120) serves as a robust tool that supports mechanistic studies across diverse biochemical, cellular, and disease-model assays.
Key Features
- Orally bioavailable RTK inhibitor
- Competitively blocks the ATP-binding pockets of VEGFR, FGFR, and PDGFR
- Modulates RTK-dependent signaling or biological activity
- Disrupts downstream signaling cascades crucial for cellular proliferation
Applications
- RTK pharmacology and target-validation studies
- IPF Modeling Benchmark (acts as a positive control drug)
- Oncology Signaling Probing
- Multi-Organ Fibrosis Screening
- Tyrosine Kinase Profiling (as a reference compound)
More Information
| Parent CAS No. | 656247-17-5 |
|---|---|
| Chemical Name | (Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate |
| SMILES | N1C2=C(C=CC(C(OC)=O)=C2)/C(=C(/NC2=CC=C(N(C)C(CN3CCN(C)CC3)=O)C=C2)C2=CC=CC=C2)/C1=O |
| MFCD | N.A. |
| InChi | InChI=1S/C31H33N5O4/c1-34-15-17-36(18-16-34)20-27(37)35(2)24-12-10-23(11-13-24)32-29(21-7-5-4-6-8-21)28-25-14-9-22(31(39)40-3)19-26(25)33-30(28)38/h4-14,19,32H,15-18,20H2,1-3H3,(H,33,38)/b29-28- |
| InChiKey | XZXHXSATPCNXJR-ZIADKAODSA-N |
| CID | 135423438 |
| Short Description | RTK inhibitor |
References
- C Rolfo et al. BIBF 1120/ nintedanib : a new triple angiokinase inhibitor-directed therapy in patients with non-small cell lung cancer. Expert Opin Investig Drugs. 2013 Aug;22(8):1081-8.
- G Bousquet et al. Phase I study of BIBF 1120 with docetaxel and prednisone in metastatic chemo-naive hormone-refractory prostate cancer patients. Br J Cancer. 2011 Nov 22;105(11):1640-5.
- F Hilberg et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82.
- GJ Roth et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). J Med Chem. 2009 Jul 23;52(14):4466-80.
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