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    BGT226 (NVP-BGT226)
    BGT226 (NVP-BGT226)

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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 #: V0131
    CAS #: 1245537-68-1Purity ≥98%

    Description: BGT226 maleate (also known as NVP-BGT226 maleate) is a novel and potent dual inhibitor of class I PI3K (phosphatidylinositol 3-kinase)/mammalian target of rapamycin (mTOR) with potential anticancer activity. It inhibits PI3Kα, PI3Kβ and PI3Kγ with IC50 values of 4 nM, 63 nM and 38 nM, respectively. 

    References: Tumour Biol. 2012 Jun;33(3):757-65; Clin Cancer Res. 2011 Nov 15;17(22):7116-26.

    Related CAS: 915020-55-2 (free base) 1245537-68-1 (maleate)

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    Molecular Weight (MW)

    650.6

    Formula

    C28H25F3N6O2.C4H4O4

    CAS No.

    1245537-68-1

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 30 mg/mL (46.11 mM)

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    Solubility (In vivo)

    30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL 

    Synonym/Chemical Name

    BGT226 maleate; BGT 226; BGT-226; NVP-BGT226; NVP-BGT-226; NVP-BGT 226; (Z)-but-2-enedioic acid;8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-piperazin-1-yl-3-(trifluoromethyl)phenyl]imidazo[4,5-c]quinolin-2-one


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    In Vitro

    Kinase Assay: BGT226 maleate (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.

     

    Cell Assay: NCI-H929, U266, RPMI-8226 and OPM2 MM cells are seeded in 96-well plates at a concentration of 1.5 × 104 cells/well in RPMI medium supplemented with 10% fetal bovine serum with or without NVP-BGT226 that is to be tested. After 36 hours, BrdU-labelling solution is added (final concentration: 10 μM), and cells are cultured for another 12 hours in a humidified atmosphere (37 °C/5% CO2). Then, the plates are centrifuged (10 min, 300 g), and the supernatants are discarded. The plates are dried at 60 °C for 2 hours. After fixation with ethanol/HCl for 30 min at -20 °C, the DNA is partially digested by nuclease treatment for 30 min at 37 °C. The cells are washed three times with medium and incubated with anti-BrdU-POD labelling solution for 30 min at 37 °C. The anti-POD solution is removed and the cells are washed three times with washing buffer. The ABTS substrate solution is added, and absorbance is measured in a microplate reader at 405 nm with a reference wave length of 490 nm.

    The anti-proliferative and pro-apoptotic effects of NVP-BGT226 are independent of bcr-abl status. The activation of the AKT/mTOR signal cascade is suppressed by NVP-BGT226 in a concentration- and time-dependent manner. Flow cytometric analysis exhibits an accumulation of cells in the G(0)-G(1) phase with concomitant loss in the S-phase. NVP-BGT226 displays potent growth-inhibitory activity against all tested cell lines including SCC4, TU183 and KB cell lines with the IC50 ranging from 7.4 to 30.1 nM. Notably, both Detroit 562 and HONE-1 cells, which express PIK3CA mutation H1047R, are still sensitive to the growth-inhibitory effect of NVP-BGT226 treatment. In addition, the sensitivity to NVP-BGT226 between HONE-1 cells and its cisplatin-resistant variant is almost identical. Results of the terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) assay and the analysis of caspase 3/7 and PARP indicates that NVP-BGT226 induces cancer cell death through an apoptosis-independent pathway. NVP-BGT226 induces autophagy as indicated by the aggregation and upregulation of the microtubule-associated protein light chain 3B-II, and p62 degradation. Gene silencing of Beclin1 or cotreatment of the autophagosome inhibitor, 3-methyladenine, inhibits the NVP-BGT226-induced autophagy and leads to the retrieval of colony survival.

    In Vivo

    In a xenografted animal model, NVP-BGT226 significantly delays tumor growth in a dose-dependent manner, along with suppressed cytoplasmic expression of p-p70 S6 kinase and the presence of autophagosome formation. NVP-BGT226 inhibits tumor growth in a dose-dependent manner in a FaDu cell xenografted mouse model. Oral administration of NVP-BGT226 at 2.5 and 5 mg/kg for 3 weeks causes 34.7% and 76.1% reduction of the tumor growth on day 21, respectively (compared with control). NVP-BGT226 displays comparable inhibition against tumor growth to rapamycin. The final volume of both groups is significantly smaller than those treated with LY294002 (a PI3K inhibitor) or the control.

    Animal model

    Human FaDu xenografted mice

    Formulation & Dosage

    Dissolved in 90% N -methyl-2-pyrrolidone (NMP)/10% PEG300.; 5 mg/kg; oral administration

    References

    [1] Markman B, et al. Ann Oncol, 2012, 23(9), 2399-2408.[2] Chang KY, et al. Clin Cancer Res, 2011, 17(22), 7116-7126.


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

    BGT226 (NVP-BGT226)

    Effect of BGT226 on intracellular signal changes in head and neck cancer cell lines.  2011 Nov 15;17(22):7116-26.

    BGT226 (NVP-BGT226)

    Effect of BGT226 on cell cycle. A, cell-cycle distribution of all tested cell lines in the presence of BGT226 or DMSO as control was evaluated by flow cytometric analysis.  2011 Nov 15;17(22):7116-26.

    BGT226 (NVP-BGT226)

    Analysis of autophagy in BGT226-treated cell lines.   2011 Nov 15;17(22):7116-26.

    BGT226 (NVP-BGT226)

    Xenograft model of FaDu cells.  2011 Nov 15;17(22):7116-26.

    BGT226 (NVP-BGT226)

    Analysis of apoptosis in BGT226-treated FaDu cells.  2011 Nov 15;17(22):7116-26.



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