1. Apoptosis
  2. Bcl-2 Family

Navitoclax (Synonyms: ABT-263)

Cat. No.: HY-10087 Purity: 99.34%
Data Sheet SDS Handling Instructions

Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds with high affinity (Ki < 1 nM) to multiple anti-apoptotic Bcl-2 family proteins including Bcl-xL, Bcl-2 and Bcl-w.

For research use only. We do not sell to patients.
Navitoclax Chemical Structure

Navitoclax Chemical Structure

CAS No. : 923564-51-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $86 In-stock
5 mg $50 In-stock
10 mg $80 In-stock
25 mg $140 In-stock
50 mg $200 In-stock
100 mg $350 In-stock
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Customer Review

    Navitoclax purchased from MCE. Usage Cited in: ACS Med Chem Lett. 2015 Jun 22;6(8):948-52.

    Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds with high affinity (Ki < 1 nM) to multiple anti-apoptotic Bcl-2 family proteins including Bcl-xL, Bcl-2 and Bcl-w.

    IC50 & Target

    Ki: < 1 nM (Bcl-xL), < 1 nM (Bcl-2), < 1 nM (Bcl-w)

    In Vitro

    Navitoclax (ABT-263) is active against approximately one-half of the cell lines of the PPTP in vitro panel. The median IC50 for all of the lines in the panel is 1.91 µM[1]. Navitoclax in combination with chemotherapy agents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation at all paclitaxel doses tested in both SK-OV-3 and IGROV-1 cell lines[2].

    In Vivo

    Navitoclax (100 mg/kg/day, p.o.) also improves responses to bendamustine-rituximab (BR) in a subset of tumours in mice xenograft[3].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.0261 mL 5.1303 mL 10.2605 mL
    5 mM 0.2052 mL 1.0261 mL 2.0521 mL
    10 mM 0.1026 mL 0.5130 mL 1.0261 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [2]

    To measure caspase-3/7 activation, IGROV-1 and SKOV3 cells are seeded in 96-well plates at 5,000 cells per well. After 24 hours, cells are treated with navitoclax (1 μM), paclitaxel (dose range=1-100 nM), or in combination with navitoclax and paclitaxel using the same dosing concentrations. Each treatment is done in duplicate wells. Induction of apoptosis, following treatment at time 0, 4, 24, and 48 hours, is determined using a Caspase-Glo 3/7 assay. A DMSO control is included in all studies. The experiment is conducted twice, and the data are presented as an average of both runs. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    Navitoclax is dissolved in DMSO.

    Cells are seeded in 384-well plates at 3,000 cells per well. After 24 hours, cells are treated with navitoclax (dose range of 14 nM-3.3 μM) and paclitaxel (dose range of 15 pM-100 nM) or gemcitabine (dose range of 0.5 nM-3.3 μM) in a 9 by 7 matrix. Each treatment is carried out in quadruplicate. Cells are treated for 72 hours, and cell viability is determined using the CellTiter-Glo assay. Cell viability for each treatment is normalized against the DMSO control group.  MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Navitoclax is administered by oral gavage once daily in a mixture of Phosal 50PG : PEG400 : ethanol.

    For systemic Granta 519 tumour models, 2×106 cells are injected via the tail vein in 0.1 mL volume of cell medium on day 0, and treatment is initiated on day 14. All animals are ear-tagged and monitored individually throughout the experiment. Navitoclax is administered by oral gavage once daily in a mixture of Phosal 50PG : PEG400 : ethanol. Bendamustine and rituximab are administered i.v. at 25 and 10 mg/kg, respectively, on day 1. Navitoclax is administered approximately 2 h before bendamustine and rituximab. All trials are comprised of 10 mice per group. Mice are humanely killed when tumours reached a size >2000 mm3 or when any signs of distress are monitored. Signs of distress include loss of ambulation, laboured breathing or weight loss > 20% mean body weight per cage. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    974.61

    Formula

    C₄₇H₅₅ClF₃N₅O₆S₃

    CAS No.

    923564-51-6

    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

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

    Purity: 99.34%

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    Inquiry Information

    Product Name:
    Navitoclax
    Cat. No.:
    HY-10087
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