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    Brivanib (BMS-540215)
    Brivanib (BMS-540215)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0506
    CAS #: 649735-46-6Purity ≥98%

    Description: Brivanib (formerly BMS-540215; BMS540215) is a novel,  investigational, oral and ATP-competitive inhibitor of VEGFR2 with potential anticancer activity. It inhibits VEGFR2 with an IC50 of 25 nM, and shows moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. It exhibits excellent anti-proliferative activity in vitro and high in vivo antitumor efficacy in H3396 xenografts in athymic mice.

    References: J Med Chem. 2006 Apr 6;49(7):2143-6; Clin Cancer Res. 2008 Oct 1;14(19):6146-53.

    Related CAS: 649735-63-7 (alaninate); 649735-46-6 

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    Molecular Weight (MW)370.38
    FormulaC19H19FN4O3
    CAS No.649735-46-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 74 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: 3 mg/mL (8.1 mM)
    SMILESC[[email protected]@H](O)COC1=CN2N=CN=C(OC3=C(F)C4=C(NC(C)=C4)C=C3)C2=C1C
    SynonymsBrivanib; BMS-540215; BMS 540215; BMS540215 

    Chemical Name: (R)-1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)oxy)propan-2-ol

    InChi Key: WCWUXEGQKLTGDX-LLVKDONJSA-N

    InChi Code: InChI=1S/C19H19FN4O3/c1-10-6-13-14(23-10)4-5-15(17(13)20)27-19-18-12(3)16(26-8-11(2)25)7-24(18)22-9-21-19/h4-7,9,11,23,25H,8H2,1-3H3/t11-/m1/s1

    SMILES Code: C[[email protected]@H](O)COC1=CN2N=CN=C(OC3=C(F)C4=C(NC(C)=C4)C=C3)C2=C1C


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    In Vitro

    In vitro activity: Brivanib also 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.


    Kinase Assay: Recombinant proteins containing tyrosine kinases are expressed as GST fusion proteins using baculovirus expression vector system in Sf9 cells. All enzymes are stored at -80 °C. Brivanib is dissolved in DMSO and diluted by water/10% DMSO. The VEGFR2 kinase solution is composed by 8 ng GST-VEGFR2 enzyme, 75 μg/mL substrate, 1 μM ATP, and 0.04 μCi [γ-33P]-ATP in 50 μL buffer: 20 mM Tris (pH 7.0), 25 μg/mL BSA, 1.5 mM MnCl2, 0.5 mM dithiothreitol). Flk-1 kinase solution is composed by 10 ng GST-Flk-1 enzyme, 75 μg/mL substrate, 1 μM ATP, and 0.04 μCi [γ-33P]-ATP in 50 μL buffer: 20 mM Tris, pH 7.0, 25 μg/mL BSA, 4 mM MnCl2, 0.5 mM dithiothreitol). The reactions are incubated for 1 hour at 27 °C and terminated with cold trichloroacetic acid (TCA) to a final concentration of 15%. These TCA precipitates are collected onto unifilter plates and quantitated by liquid scintillation counter.


    Cell Assay: The cells are stimulated by VEGF or FGF at a concentration of 8 or 80 ng/mL. These cells are seeded in 96 well plates at a density of 2 × 103and incubated for 24 hours. Brivanib at various dilutions are added to the cells for another 48 hours. Then 0.5 μCi of [3H] thymidine is added for 24 hours. After that the incorporated tritium is quantified using a β-counter.

    In VivoBrivanib 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. 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.
    Animal modelH3396 xenografts in athymic mice
    Formulation & DosageDissolved in PEG400: Tween80 (75:25) (orally) or PEG400: water (3:2) (i.v.); 1mg/kg; oral gavage or i.v.
    References

    J Med Chem. 2006 Apr 6;49(7):2143-6; Clin Cancer Res. 2008 Oct 1;14(19):6146-53.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Brivanib (BMS-540215)

    Effects of brivanib on growth rate of patient-derived HCC xenograft lines 06-0606, 2-1318, and 26-1004. Clin Cancer Res. 2008 Oct 1;14(19):6146-53.

    Brivanib (BMS-540215)

    Effects of brivanib on VEGFR-2 activity, cell proliferation, and apoptosis in HCC xenograft lines 06-0606 (A) and 26-1004 (B). Clin Cancer Res. 2008 Oct 1;14(19):6146-53.

    Brivanib (BMS-540215)

    Effects of brivanibon (A and C) VEGF-induced, bFGF-induced, and (B) IGF-I–induced phosphorylation of VEGFR-2, FGFR, Akt, and ERK1/2 in SK-HEP1 (A and B) and HepG2 (C) cells. Clin Cancer Res. 2008 Oct 1;14(19):6146-53.


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