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

Nintedanib esylate (Synonyms: BIBF 1120 esylate)

Cat. No.: HY-11106 Purity: 99.95%
Handling Instructions

Nintedanib esylate (BIBF 1120 esylate) 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 esylate Chemical Structure

Nintedanib esylate Chemical Structure

CAS No. : 656247-18-6

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10 mM * 1 mL in DMSO USD 73 In-stock
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100 mg USD 132 In-stock
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200 mg USD 204 In-stock
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500 mg USD 408 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Nintedanib esylate:

Top Publications Citing Use of Products

    Nintedanib esylate purchased from MCE. Usage Cited in: Sci Rep. 2018 Jun 22;8(1):9540.

    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 esylate 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).

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Nintedanib esylate (BIBF 1120 esylate) 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)

    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].

    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].

    Clinical Trial
    Molecular Weight

    649.76

    Formula

    C₃₃H₃₉N₅O₇S

    CAS No.

    656247-18-6

    SMILES

    O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(N(C)C(CN4CCN(C)CC4)=O)C=C3)/C5=CC=CC=C5)OC.CCS(=O)(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 92.85 mg/mL (142.90 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5390 mL 7.6951 mL 15.3903 mL
    5 mM 0.3078 mL 1.5390 mL 3.0781 mL
    10 mM 0.1539 mL 0.7695 mL 1.5390 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    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[1].

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

    References

    Purity: 99.95%

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    Nintedanib esylate
    Cat. No.:
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