Target Selectivity of BIBF 1120 (Nintedanib)
| Key Target | IC50 | Description | Reference |
|---|---|---|---|
| Human VEGFR2 | 7 nM | TKI activity assay | PMC12519263 |
| VEGFR2 | 13 nM | competitively binds to ATP binding pocket of kinases to block intracellular signalling cascades | PMC13005838 |
| VEGFR1 | 13 nM | competitively binds to ATP binding pocket of kinases to block intracellular signalling cascades | PMC13005838 |
| VEGFR3 | 13 nM | competitively binds to ATP binding pocket of kinases to block intracellular signalling cascades | PMC13005838 |
| VEGFR-1 | 13 nM | Kinase inhibition assay | PMC3693725 |
| VEGFR-2 | 13 nM | Kinase inhibition assay | PMC3693725 |
| VEGFR-3 | 13 nM | Kinase inhibition assay | PMC3693725 |
| VEGFR | 13 nM | Biochemical assay (implied) | PMC10206228 |
| FGFR | 13 nM | Biochemical assay (implied) | PMC10206228 |
| PDGFR | 13 nM | Biochemical assay (implied) | PMC10206228 |
| VEGFR | 13 nM | enzymatic assays | PMC4801128 |
| FLT3 | 16 nM | inhibits receptor tyrosine kinase | PMC13005838 |
| LCK | 16 nM | inhibits non-receptor tyrosine kinases | PMC13005838 |
| LYN | 16 nM | inhibits non-receptor tyrosine kinases | PMC13005838 |
| SRC | 16 nM | inhibits non-receptor tyrosine kinases | PMC13005838 |
| FGFR1 | 37 nM | competitively binds to ATP binding pocket of kinases to block intracellular signalling cascades | PMC13005838 |
| FGFR2 | 37 nM | competitively binds to ATP binding pocket of kinases to block intracellular signalling cascades | PMC13005838 |
| FGFR3 | 37 nM | competitively binds to ATP binding pocket of kinases to block intracellular signalling cascades | PMC13005838 |
| FGFR-1 | 37 nM | Kinase inhibition assay | PMC3693725 |
| FGFR-2 | 37 nM | Kinase inhibition assay | PMC3693725 |
| FGFR-3 | 37 nM | Kinase inhibition assay | PMC3693725 |
| FGF receptor | 37 nM | enzymatic assays | PMC4801128 |
| PDGF receptor (R)-α | 59 nM | Kinase inhibition assay | PMC3693725 |
| PDGFRα | 59 nM | competitively binds to ATP binding pocket of kinases to block intracellular signalling cascades | PMC13005838 |
| PDGF receptor | 59 nM | enzymatic assays | PMC4801128 |
| PDGF receptor (R)-β | 65 nM | Kinase inhibition assay | PMC3693725 |
| PDGFRβ | 65 nM | competitively binds to ATP binding pocket of kinases to block intracellular signalling cascades | PMC13005838 |
Check the
BIBF 1120 (Nintedanib)
product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.
Cell-free Assays (IC50/Ki) for BIBF 1120 (Nintedanib)
| Key Target | IC50 (Cell-free) | Description | Reference |
|---|---|---|---|
| Human recombinant VEGFR2 | 7 nM | TKI activity assay | Download PDF |
| VEGFR2 | 7 nM | Radiometric detection method | Download PDF |
| VEGFR2 | 7 nM | enzymatic radiometric assay (using [γ-33P]-ATP) | PMC9161413 |
| VEGFR, FGFR, PDGFR | 13–34 nM (VEGF), 37–108 nM (FGF), 59–65 nM (PDGF) | Biochemical assay (implied) | Download PDF |
| PDGF receptor (R)-α | 59 nmol/L | Kinase inhibition assay | PMC3693725 |
| PDGF receptor (R)-β | 65 nmol/L | Kinase inhibition assay | PMC3693725 |
| VEGFR-1, -2, -3 | 13–34 nmol/L | Kinase inhibition assay | PMC3693725 |
| FGFR-1, -2, -3 | 37–108 nmol/L | Kinase inhibition assay | PMC3693725 |
| VEGFR, PDGF receptor, FGF receptor | VEGFR: 13 nM, PDGF receptor: 59 nM, FGF receptor: 37 nM | enzymatic assays | PMC4801128 |
Cell-based Assay (IC50) for BIBF 1120 (Nintedanib)
| Cell Type | IC50 (Cell-based) | Description | Reference |
|---|---|---|---|
| RPE cells | 18.8 mM (NTB-PBS), 29.5 mM (NTB-LIP) | MTT method | PMC12085219 |
| IPF FBs | 4.16 µM | MTT assay | Download PDF |
| HPFs | 2.38 µM | MTT assay | Download PDF |
| AGS cells | 5.3 ± 0.9 mM | CCK-8 assay | Download PDF |
| MKN28 cells | 6.1 ± 1.2 mM | CCK-8 assay | Download PDF |
| AGS | 6.51 ± 0.49 µM | CCK-8 assay | Download PDF |
| MKN-28 | 8.07 ± 0.13 µM | CCK-8 assay | Download PDF |
| HCT116 wildtype | 8.2 µM | Resazurin assay | Download PDF |
| HCT116 wildtype | 8.2 µM | Resazurin assay | Download PDF |
| Fibrotic mouse lung PCLSs | 897 nM | Reduction of Col1a1 mRNA levels by 50% in fibrotic mouse lung PCLSs | Download PDF |
| PDAC CAFs | 9.76 to 40.84 µM | Cell viability assay | PMC9972461 |
| PBMCs | 28 nmol/L | Cytokine-specific detection antibody labeled with MSD SULFO-TAG™ reagent by a Meso Scale SECTOR imager, followed by non-linear fitting. | PMC7954282 |
| PAN-T cells | 53 nmol/L | Cytokine-specific detection antibody labeled with MSD SULFO-TAG™ reagent by a Meso Scale SECTOR imager, followed by non-linear fitting. | PMC7954282 |
| CD4+ T cells | 48 nmol/L | Cytokine-specific detection antibody labeled with MSD SULFO-TAG™ reagent by a Meso Scale SECTOR imager, followed by non-linear fitting. | PMC7954282 |
| CD8+ T cells | 73 nmol/L | Cytokine-specific detection antibody labeled with MSD SULFO-TAG™ reagent by a Meso Scale SECTOR imager, followed by non-linear fitting. | PMC7954282 |
| CBMCs | 13.7 nM | Flow cytometry for viable ckit-positive MCs | PMC7476277 |
| CBMCs (ckit phosphorylation) | 13.3 nM | Electrochemiluminescence-based phospho-ckit assay | PMC7476277 |
| CBMCs | 14.8 nM | 3H-thymidine incorporation | PMC7476277 |
| NHLFs | 526 nM | 3H-thymidine incorporation | PMC7476277 |
| Control fibroblasts | 0.93 ±0.09 mM | Fold cell number assay, data fitted to an exponential decay function | PMC5674098 |
| Control fibroblasts | 1.1±0.3 mM | COL1A1 expression assay, data fitted to an exponential decay function | PMC5674098 |
| ADC-TAFs | 0.96 ±0.09 mM | Fold cell number assay, data fitted to an exponential decay function | PMC5674098 |
| ADC-TAFs | 1.05 ±0.07 mM | COL1A1 expression assay, data fitted to an exponential decay function | PMC5674098 |
| SCC-TAFs | 1.09 ±0.05 mM | Fold cell number assay, data fitted to an exponential decay function | PMC5674098 |
| SCC-TAFs | 2.3 ±0.6 mM | COL1A1 expression assay, data fitted to an exponential decay function | PMC5674098 |
| DMS114 | 1.97 ± 0.31 μM | MTT assay, non-linear regression curve-fitting (sigmoidal dose-response with variable slope) | Download PDF |
| NCI-H520 | 6.67 ± 4.20 μM | MTT assay, non-linear regression curve-fitting (sigmoidal dose-response with variable slope) | Download PDF |
| NCI-H1703 | 0.98 ± 0.33 μM | MTT assay, non-linear regression curve-fitting (sigmoidal dose-response with variable slope) | Download PDF |
| HNE-1 | 4.16 ±0.04 µM | Cell Counting Kit 8 assay | PMC4801128 |
| CNE-2 | 5.62±2.64 µM | Cell Counting Kit 8 assay | PMC4801128 |
| HONE-1 | 6.32 ±1.18 µM | Cell Counting Kit 8 assay | PMC4801128 |
Jump to
- BIBF 1120 (Nintedanib) Mechanism of Action: PDGFR Inhibition in Lung Fibroblast Research
- BIBF 1120 (Nintedanib) Clinical Trials
- BIBF 1120 (Nintedanib) Working Concentration | Cell Culture | Treatment
- BIBF 1120 (Nintedanib) Solubility in DMSO
- BIBF 1120 (Nintedanib) Stock Solution
- BIBF 1120 (Nintedanib) Storage
- BIBF 1120 (Nintedanib) Stability
- BIBF 1120 (Nintedanib) Combination Database
- BIBF 1120 (Nintedanib) Molecular Weight
- BIBF 1120 (Nintedanib) SMILES
- BIBF 1120 (Nintedanib) CAS Number
- BIBF 1120 (Nintedanib) Chemical Structure (2D and 3D)
- BIBF 1120 (Nintedanib) IC50 for Cell-based and Cell-free Assays
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