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

Navitoclax  (Synonyms: ABT-263)

製品番号: HY-10087 純度: 99.72%
COA 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
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 75 在庫あり
Solution
10 mM * 1 mL in DMSO USD 75 在庫あり
Solid
5 mg USD 50 在庫あり
10 mg USD 70 在庫あり
50 mg USD 180 在庫あり
100 mg USD 250 在庫あり
500 mg USD 800 在庫あり
1 g   お問い合わせ  
5 g   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

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カスタマーレビュー

Based on 72 publication(s) in Google Scholar

Other Forms of Navitoclax:

Top Publications Citing Use of Products

顧客検証

Proliferation Assay
WB

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

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

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

    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.

    Bcl-2 Family アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    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[1].

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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
    Appearance

    Solid

    Color

    White to light yellow

    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[C@H](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)

    *"≥" 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:  60% phosal 50 propylene glycol (PG), 30% polyethylene glycol 400 (PEG400), 10% ethanol

      Solubility: 7.5 mg/mL (7.70 mM); Clear solution; Need ultrasonic

    • 2.

      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

    • 3.

      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

    • 4.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    *All of the co-solvents are available by MedChemExpress (MCE).
    純度とドキュメンテーション

    純度: 99.97% ee.: 99.92%

    参考文献
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    Navitoclax Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    • モル濃度カルキュレーター

    • 希釈カルキュレーター

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

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