1. Protein Tyrosine Kinase/RTK
  2. PDGFR VEGFR FGFR
  3. Nintedanib

Nintedanib  (Synonyms: BIBF 1120)

Cat. No.: HY-50904 Purity: 99.90%
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Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

For research use only. We do not sell to patients.

Nintedanib Chemical Structure

Nintedanib Chemical Structure

CAS No. : 656247-17-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
10 mg USD 66 In-stock
50 mg USD 96 In-stock
100 mg USD 132 In-stock
200 mg USD 204 In-stock
500 mg USD 408 In-stock
1 g USD 660 In-stock
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Customer Review

Based on 50 publication(s) in Google Scholar

Other Forms of Nintedanib:

Top Publications Citing Use of Products

48 Publications Citing Use of MCE Nintedanib

WB
Proliferation Assay

    Nintedanib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Jun 22;8(1):9540.  [Abstract]

    Western blot based detection of cell cycle associated molecules viz., Cyclins A, D1 and E, and CDKs 2, 4 and 6 in PC3, and LNCaP cells after 72 hours of Nintedanib treatment.

    Nintedanib purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2016 Dec;36(6):3123-3130.  [Abstract]

    The mice are treated with TFTD alone (150 mg/kg, orally twice daily from days 1 to 14, open column), or a combination of TFTD and Nintedanib (closed column). The HT-29 and HCT116 tumors are collected at 24 h following the final administration of the drugs (day 15). The values indicate the mean ± SD (n=6).

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

    IC50 & Target[1]

    VEGFR1

    34 nM (IC50)

    VEGFR2

    13 nM (IC50)

    VEGFR3

    13 nM (IC50)

    FGFR1

    69 nM (IC50)

    FGFR2

    37 nM (IC50)

    FGFR3

    108 nM (IC50)

    PDGFRα

    59 nM (IC50)

    PDGFRβ

    65 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    22.62 μM
    Compound: Nintedanib
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 28826084]
    Calu-6 EC50
    > 1 μM
    Compound: 3, BIBF1120
    Antiangiogenic activity against human Calu6 cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay
    Antiangiogenic activity against human Calu6 cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay
    [PMID: 19522465]
    Calu-6 EC50
    > 3500 nM
    Compound: BIBF 1120
    Antiangiogenic activity in human Calu6 assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum
    Antiangiogenic activity in human Calu6 assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum
    [PMID: 18559524]
    FaDu EC50
    > 1 μM
    Compound: 3, BIBF1120
    Antiangiogenic activity against human FADU cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay
    Antiangiogenic activity against human FADU cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay
    [PMID: 19522465]
    FaDu EC50
    > 4500 nM
    Compound: BIBF 1120
    Antiangiogenic activity in human FADU assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum
    Antiangiogenic activity in human FADU assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum
    [PMID: 18559524]
    HeLa EC50
    > 1 μM
    Compound: 3, BIBF1120
    Antiangiogenic activity against human HeLa cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay
    Antiangiogenic activity against human HeLa cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay
    [PMID: 19522465]
    HeLa EC50
    > 3500 nM
    Compound: BIBF 1120
    Antiangiogenic activity in human HeLa assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum
    Antiangiogenic activity in human HeLa assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum
    [PMID: 18559524]
    HeLa IC50
    51.65 μM
    Compound: Nintedanib
    Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
    [PMID: 28190652]
    HT-29 IC50
    0.83 μM
    Compound: Nintedanib
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    [PMID: 28826084]
    HT-29 IC50
    4.9 μM
    Compound: Nintedanib
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    [PMID: 28190652]
    HUVEC EC50
    < 10 nM
    Compound: BIBF 1120
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced apoptosis by [3H]thymidine incorporation assay
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced apoptosis by [3H]thymidine incorporation assay
    [PMID: 18559524]
    HUVEC IC50
    10 nM
    Compound: 3, BIBF1120
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay
    [PMID: 19522465]
    HUVEC EC50
    290 nM
    Compound: BIBF 1120
    Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation by [3H]thymidine incorporation assay
    Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation by [3H]thymidine incorporation assay
    [PMID: 18559524]
    HUVEC EC50
    9 nM
    Compound: BIBF 1120
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay
    [PMID: 18559524]
    MCF7 IC50
    8.28 μM
    Compound: Nintedanib
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 28826084]
    NRK-49F IC50
    1.1 μM
    Compound: Nintedanib
    Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis
    Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis
    [PMID: 32334267]
    NRK-49F IC50
    1.1 μM
    Compound: 2
    Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis
    Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis
    [PMID: 31699535]
    PC-3 IC50
    < 30 μM
    Compound: Nintedanib
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability by CellTiter-Fluor assay
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability by CellTiter-Fluor assay
    [PMID: 30951312]
    Sf9 IC50
    1.9 nM
    Compound: BIBF 1120
    Inhibition of N-terminal GST-tagged human recombinant PDGFRalpha D842I mutant expressed in baculovirus-infected Sf9 cells using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobilit
    Inhibition of N-terminal GST-tagged human recombinant PDGFRalpha D842I mutant expressed in baculovirus-infected Sf9 cells using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobilit
    [PMID: 32305182]
    Sf9 IC50
    13 nM
    Compound: BIBF 1120
    Inhibition of mouse GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting
    Inhibition of mouse GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting
    [PMID: 18559524]
    Sf9 IC50
    21 nM
    Compound: BIBF 1120
    Inhibition of human GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting
    Inhibition of human GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting
    [PMID: 18559524]
    SK-OV-3 IC50
    28.76 μM
    Compound: Nintedanib
    Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay
    [PMID: 28190652]
    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)[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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[1]. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    539.62

    Formula

    C31H33N5O4

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1NC2=CC(C(OC)=O)=CC=C2/C1=C(NC3=CC=C(N(C(CN4CCN(C)CC4)=O)C)C=C3)\C5=CC=CC=C5

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 5.83 mg/mL (10.80 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8532 mL 9.2658 mL 18.5316 mL
    5 mM 0.3706 mL 1.8532 mL 3.7063 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (18.53 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  1% CMC/0.5% Tween-80 in Saline water

      Solubility: 10 mg/mL (18.53 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.94%

    References
    Kinase Assay
    [2]

    Enzyme activity is assayed in the presence or absence of serial dilutions of BIBF1120 performed in 25% DMSO. Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound. All incubations are conducted at room temperature on a rotation shaker. 10 μL of each BIBF1120 dilution is added to 10 μL of diluted kinase (0.8 μg/mL VEGFR2, 10 mM Tris pH 7.5, 2 mM EDTA, and 2 mg/mL BSA) and preincubated for 1 hour. The reaction is started by addition of 30 μL of substrate mix containing 62.4 mM Tris pH 7.5, 2.7 mM DTT, 5.3 mM MnCl2, 13.3 mM Mg-acetate, 0.42 mM ATP, 0.83 mg/mL Poly-Glu-Tyr(4:1), and 1.7 μg/mL Poly-Glu-Tyr(4:1)-biotin and incubated for 1 hour. The reaction is stopped by addition of 50 μL of 250 mM EDTA, 20 mM HEPES, pH 7.4. 90 μL of the reaction mix is transferred to a streptavidin plate and incubated for 1-2 hours. After three washes with PBS the EU-labeled antibody, PY20 is added (recommended dilution 1:2000 of 0.5 mg/mL labeled antibody in DELFIA assay buffer). Excessive detection antibody is removed by three ishes of DELFIA washing buffer. Then 10 minutes before measurement on the multilabel reader, each well is incubated with 100 μL of DELFIA enhancement solution.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Five-week-old to 6-wk-old athymic NMRI-nu/nu female mice (21-31 g) are used for the assay. After acclimatization, mice are inoculated with 1 to 5×106 (in 100 μL) FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 cells s.c. into the right flank of the animal. After acclimatization, F344 Fischer rats are injected with 5×106 (in 100 μL) GS-9L cells s.c. into the right flank of the animal. For pharmacokinetic analysis, blood is isolated at indicated time points from the retroorbital plexus of mice and plasma is analyzed using high performance liquid chromatography-mass spectrometry methodology.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8532 mL 9.2658 mL 18.5316 mL 46.3289 mL
    5 mM 0.3706 mL 1.8532 mL 3.7063 mL 9.2658 mL
    10 mM 0.1853 mL 0.9266 mL 1.8532 mL 4.6329 mL
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