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

Navitoclax (Synonyms: ABT-263)

目录号: HY-10087 纯度: 99.80%
产品使用指南

Navitoclax (ABT-263) 是有效,可口服的 Bcl-2 抑制剂,可与Bcl-xL,Bcl-2, Bcl-w等多种Bcl-2家族蛋白结合,Ki 值小于 1 nM。

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Navitoclax Chemical Structure

Navitoclax Chemical Structure

CAS No. : 923564-51-6

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10 mM * 1 mL in DMSO ¥1029
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5 mg ¥650
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10 mg ¥960
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50 mg ¥2500
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100 mg ¥3500
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 44 篇科研文献

    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.

    查看 Bcl-2 Family 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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)

    体外研究
    (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].

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

    体内研究
    (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].

    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.
    Clinical Trial
    分子量

    974.61

    Formula

    C47H55ClF3N5O6S3

    CAS 号
    中文名称

    生根粉263

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMF : ≥ 100 mg/mL (102.61 mM)

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

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 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

    • 2.

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: 5.5 mg/mL (5.64 mM); Suspended solution; Need ultrasonic

    • 3.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

      此方案可获得 2.08 mg/mL (2.13 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 4.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

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

      此方案可获得 2.08 mg/mL (2.13 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 5.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

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

      此方案可获得 ≥ 2.08 mg/mL (2.13 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献

    纯度: 99.97% ee.: 99.92%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    目录号:
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