1. Apoptosis
  2. Bcl-2 Family
  3. Navitoclax

Navitoclax (Synonyms: ABT-263)

Cat. No.: HY-10087 Purity: 99.97% ee.: 99.92%
Handling Instructions

Navitoclax (ABT-263) est un protéine de la famille Bcl-2 puissant et actif par voie orale qui se lie à de multiples protéines anti-apoptotiques de la famille Bcl-2, telles que Bcl-xL, Bcl-2 et Bcl-w, avec un Ki inférieur à 1 nM.

Navitoclax (ABT-263) ist ein wirksamer und oral wirksamer Proteininhibitor der Bcl-2-Familie, der an mehrere antiapoptotische Proteine ​​der Bcl-2-Familie wie Bcl-xL, Bcl-2 und Bcl-w mit einem Ki von weniger bindet als 1 nM.

Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM.

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

Navitoclax Chemical Structure

Navitoclax Chemical Structure

CAS No. : 923564-51-6

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10 mM * 1 mL in DMSO USD 75 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 70 In-stock
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50 mg USD 180 In-stock
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100 mg USD 250 In-stock
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Customer Review

Based on 21 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    Navitoclax purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Sep 24;9(10):986.

    Cells are treated with 25 nM siRNA for 48 hours followed by 1 μM ABT-263 for 36 hours.

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    Description

    Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM[1].

    IC50 & Target

    Bcl-W

    1 nM (Ki)

    Bcl-xL

    1 nM (Ki)

    Bcl-2

    1 nM (Ki)

    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 in both SK-OV-3 and IGROV-1 cell lines[2].

    In Vivo

    Navitoclax (100 mg/kg; orally; 21-day treatment) enhances the activity of OSI-744 in vivo. As a single agent, 100 mg/kg Navitoclax alone dosed daily has no significant antitumor activity, whereas daily dosing of OSI-744 at 50 mg/kg results in significant tumor stasis (%TGI=52) during a 21-day treatment period. Notably, the combination of Navitoclax and OSI-744 dosed daily for 21 consecutive days results in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice[3].

    Animal Model: Mice with NCI-H1650 model[3]
    Dosage: 100 mg/kg
    Administration: Orally; daily; for 21 consecutive days
    Result: As a single agent, 100 mg/kg alone dosed daily had no significant antitumor activity. Notably, the combination with OSI-744 resulted in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice.
    Clinical Trial
    Molecular Weight

    974.61

    Formula

    C₄₇H₅₅ClF₃N₅O₆S₃

    CAS No.

    923564-51-6

    SMILES

    O=S(C1=CC(S(NC(C2=CC=C(N3CCN(CC4=C(CCC(C)(C4)C)C5=CC=C(Cl)C=C5)CC3)C=C2)=O)(=O)=O)=CC=C1N[[email protected]](CCN6CCOCC6)CSC7=CC=CC=C7)(C(F)(F)F)=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: 

    DMF : ≥ 100 mg/mL (102.61 mM)

    DMSO : 75 mg/mL (76.95 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

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

      Solubility: 2.08 mg/mL (2.13 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: 2.08 mg/mL (2.13 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (2.13 mM); Clear solution

    • 4.

      Add each solvent one by one:  60% phosal 50 propylene glycol (PG), 30% polyethylene glycol 400 (PEG400), 10% ethanol

      Solubility: 12.5 mg/mL (12.83 mM); Suspended solution; Need ultrasonic

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

    Purity: 99.97% ee.: 99.92%

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    Keywords:

    NavitoclaxABT-263ABT263ABT 263Bcl-2 FamilyInhibitorinhibitorinhibit

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    Cat. No.:
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