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

Navitoclax (Synonyms: ABT-263)

製品番号: HY-10087 純度: 99.97% ee.: 99.92%
取扱説明書

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.

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Navitoclax 構造式

Navitoclax 構造式

CAS 番号 : 923564-51-6

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 75 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 70 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 180 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 250 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 9 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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    製品説明

    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.

    IC50 & Target[1]

    Bcl-W

    1 nM (Ki)

    Bcl-xL

    1 nM (Ki)

    Bcl-2

    1 nM (Ki)

    体外実験

    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].

    体内実験

    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.
    臨床実験
    分子量

    974.61

    分子式

    C₄₇H₅₅ClF₃N₅O₆S₃

    CAS 番号

    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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.
    体内:
    • 1.

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

      Solubility: 2.5 mg/mL (2.57 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (2.57 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献

    純度: 99.97% ee.: 99.92%

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    The molarity calculator equation

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

    Keywords:

    NavitoclaxABT-263ABT263ABT 263Bcl-2 FamilyInhibitorinhibitorinhibit

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    製品名:
    Navitoclax
    製品番号:
    HY-10087
    数量:
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