2. Protein Tyrosine Kinase/RTK
    Autophagy
  3. VEGFR
    Autophagy
  4. Brivanib

Brivanib  (Synonyms: BMS-540215)

Cat. No.: HY-10337 Purity: 98.24%
COA Handling Instructions

Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.

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

Brivanib Chemical Structure

Brivanib Chemical Structure

CAS No. : 649735-46-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 160 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 160 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 145 In-stock
Estimated Time of Arrival: December 31
10 mg USD 238 In-stock
Estimated Time of Arrival: December 31
50 mg USD 779 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1307 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Brivanib:

Top Publications Citing Use of Products

    Brivanib purchased from MCE. Usage Cited in: Cell Rep. 2023 Mar 20;42(3):112275.  [Abstract]

    Brivanib (0.1, 1, 10 µM) markedly increases interactions of biotin-ISD with purified SUMO-cGAS in a dose-dependent manner, in Patient-derived tumor-like cell clusters (PTCs).

    View All VEGFR Isoform Specific Products:

    View All Isoforms
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β[1].

    IC50 & Target[1]

    VEGFR2

    25 nM (IC50)

    In Vitro

    Brivanib inhibits VEGFR1 and FGFR-1 with IC50 of 0.38 μM and 0.148 μM. Brivanib is not sensitive to PDGFRβ, EGFR, LCK, PKCα or JAK-3 with IC50 all above 1900 nM. Brivanib could inhibit the proliferation of VEGF-stimulated HUVECs with IC50 of 40 nM, compared to 276 nM in FGF-stimulated HUVECs. On the other hand, brivanib exhibits low activity to tumor cell lines[1]. Brivanib doses ≤20 µM paradoxically enhances FGF-induced LX-2 cell proliferation, whereas higher brivanib doses (≥30 µM) inhibits LX-2 cell proliferation. The inhibitory effect of brivanib on liver fibrosis is not through inhibition of TGF-β1-induced stellate cell activation, and is possibly through inhibition of PDGF-BB-induced stellate cell activation[3].

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

    Brivanib displays antitumor activities in H3396 xenograft in athymic mice. At a dose of 60 and 90 mg/kg (p.o.), brivanib completely inhibits the tumor growth, with TGI of 85% and 97%, respectively[1]. Moreover, brivanib significantly suppresses tumor growth in Hepatocellular carcinoma (HCC) xenografts, which due to the decrease in phosphorylation of VEGFR2. The results show that the tumor weights in 06-0606 xenograft mice are 55% and 13%, compared with the controls at a dose of 50 mg/kg and 100 mg/kg. Brivanib is suggested to be efficient in treatment of HCC[2]. Brivanib (50 mg/kg, p.o.) attenuates liver fibrosis and stellate cell activation induced by BDL in mice. Brivanib inhibits growth factor and growth factor receptor mRNA expression in sham control animals but shows variable effects in bile duct ligated animals[3].

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

    370.38

    Appearance

    Solid

    Formula

    C19H19FN4O3
    CAS No.
    SMILES

    FC1=C(OC2=NC=NN3C2=C(C(OC[[email protected]](O)C)=C3)C)C=CC4=C1C=C(C)N4
    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 : ≥ 50 mg/mL (135.00 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6999 mL 13.4996 mL 26.9993 mL
    5 mM 0.5400 mL 2.6999 mL 5.3999 mL
    10 mM 0.2700 mL 1.3500 mL 2.6999 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: ≥ 2.08 mg/mL (5.62 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.24%

    COA (250 KB) HNMR (190 KB) LCMS (407 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [3]

    Viability is measured in LX-2 cells using the Cell Counting Kit-8 (CCK-8). Using 96-well plates with 2,000 cells per well, HSCs are incubated in 10% FBS-supplemented DMEM for 24 hours, followed by starvation in serum-free media. After 24 hours of starvation, brivanib is added at different doses. Two hours later, 5 ng/mL PDGF-BB is added. The cells are incubated for an additional 72 hours and cell viability is measured. Each experiment is performed in three replicates at least four times.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Male mice 4-6 weeks of age are treated 3 times a week with a total of 12 intraperitoneal (i.p.) injections of 150 mL/kg TAA. At the onset of TAA treatment, placebo or brivanib (25 or 50 mg/kg) is administered orally on 5 consecutive days with weekend breaks. The animals are sacrificed 4 weeks after the start of the injections.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Brivanib649735-46-6BMS-540215BMS540215BMS 540215VEGFRAutophagyVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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