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

BIBF 1120 (Synonyms: Nintedanib)

Cat. No.: HY-50904 Purity: 99.75%
Data Sheet SDS Handling Instructions

BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3FGFR1/2/3 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.
BIBF 1120 Chemical Structure

BIBF 1120 Chemical Structure

CAS No. : 656247-17-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $61 In-stock
10 mg $55 In-stock
50 mg $80 In-stock
100 mg $110 In-stock
200 mg $170 In-stock
500 mg $340 In-stock
1 g $550 In-stock
5 g   Get quote  
10 g   Get quote  

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Customer Review

Other Forms of BIBF 1120:

    BIBF 1120 purchased from MCE. Usage Cited in: Oncol Rep. 2016 Dec;36(6):3123-3130.

    The concentration of Trifluridine incorporated in the DNA in the human colorectal HT-29 (A) and HCT116 (B) xenografts. 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).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3FGFR1/2/3 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

    IC50: 34 nM (VEGFR1), 13 nM (VEGFR2), 13 nM (VEGFR3), 69 nM (FGFR1), 37 nM (FGFR1), 108 nM (FGFR1), 59 nM (PDGFRα), 65 nM (PDGFRβ)

    In Vitro

    BIBF 1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC)[1].

    In Vivo

    BIBF1120 (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]. BIBF1120 is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated[2].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.1853 mL 0.9266 mL 1.8532 mL
    Please refer to the solubility information to select the appropriate solvent.
    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]

    BIBF 1120 is formulated in a 0.5 % Natrosol solution.

    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
    Molecular Weight

    539.62

    Formula

    C₃₁H₃₃N₅O₄

    CAS No.

    656247-17-5

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    BIBF 1120 (Nintedanib) is prepared in vehicle solution that consists of 0.5% HPMC solution[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.75%

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    Product Name:
    BIBF 1120
    Cat. No.:
    HY-50904
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