Brusatol(Synonyms: 鸦胆子苦醇; NSC 172924)

发表于由

上海金畔生物科技有限公司提供天然产物萜类及其苷类Terpenoids and Glycosides。

Brusatol (Synonyms: 鸦胆子苦醇; NSC 172924) 纯度: 99.89%

Brusatol (NSC 172924) 是一种独特的 Nrf2 通路抑制剂，可使多种癌细胞对 Cisplatin 和其他化疗药物敏感。Brusatol 通过抑制 Nrf2 介导的防御机制来增强化疗的疗效。Brusatol 可开发为辅助化疗化合物。 Brusatol 增加细胞凋亡(apoptosis)。

Brusatol(Synonyms: 鸦胆子苦醇; NSC 172924)

Brusatol Chemical Structure

CAS No. : 14907-98-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2176 In-stock
2 mg ￥1100 In-stock
5 mg ￥1900 In-stock
10 mg ￥3400 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Brusatol 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Terpenoids Library
  • Traditional Chinese Medicine Monomer Library
  • Transcription Factor Targeted Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Brusatol (NSC 172924) is a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells to Cisplatin and other chemotherapeutic agents. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Brusatol can be developed into an adjuvant chemotherapeutic agent[1]. Brusatol increases cellular apoptosis[2].

IC50 & Target

Nrf2[1]
体外研究
(In Vitro)

Brusatol (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) reduces the viability of CT-26 cells in a dose-dependent manner with IC50 value of 0.27±0.01μg/mL. When Brusatol is combined with Cisplatin (CDDP) at a constant concentration ratio of 1:1, cell growth inhibition is markedly enhanced compared with single-agent treatment; the IC50 value of Brusatol and CDDP cotreatment is 0.19±0.02μg/mL[2].
Brusatol provokes a rapid and transient depletion of Nrf2 protein, through a posttranscriptional mechanism, in mouse Hepa-1c1c7 hepatoma cells. Brusatol sensitizes mammalian cells to chemical toxicity-implications for therapeutic targeting of Nrf2[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: The murine CT-26 CRC cell line
Concentration: 0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL
Incubation Time: 48 hours
Result: The viability of CT-26 cells was reduced in a dose-dependent manner, with IC50 value of 0.27±0.01 μg/mL.

Western Blot Analysis[3]

Cell Line: Mouse Hepa-1c1c7 hepatoma cells
Concentration: 1, 3, 10, 30, 100, 300, and 1000 nM
Incubation Time: 2 hours
Result: Provoked the depletion of Nrf2, in a concentration-dependent manner within 2 h of exposure to cells.

体内研究
(In Vivo)

“Brusatol is able to reach the tumor tissue and inhibit the Nrf2 pathway. Nude mice are injected with A549 cells to induce tumor growth, followed by a single i.p. injection of 2 mg/kg Brusatol. Nrf2 protein levels are significantly decreased at 24 h or 48 h postinjection[1]. 
Cisplatin (2 mg/kg) or Brusatol (2 mg/kg) alone does not inhibit tumor growth significantly, whereas in the combination group, tumor size is significantly reduced[1]. “

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Athymic nude mice 4-6 wk old bearing A549 xenografts[1]
Dosage: 2 mg/kg
Administration: Treated i.p.; Cisplatin (2 mg/kg), Brusatol (2 mg/kg), or in combination every other day for a total of five times
Result: Nrf2 protein levels were significantly decreased at 24 h or 48 h postinjection.
Cisplatin or Brusatol alone did not inhibit tumor growth significantly, whereas in the combination group, tumor size was significantly reduced. ”

分子量

520.53

Formula

C26H32O11
CAS 号

14907-98-3
中文名称

鸦胆子苦醇；鸦胆苦醇
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (48.03 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9211 mL 9.6056 mL 19.2112 mL
5 mM 0.3842 mL 1.9211 mL 3.8422 mL
10 mM 0.1921 mL 0.9606 mL 1.9211 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 (protect from light, stored under nitrogen)。-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： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.80 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.80 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.80 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 25.0 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Dongmei Ren, et al. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Proc Natl Acad Sci U S A. 2011 Jan 25;108(4):1433-8.

    [2]. Hai-Ming Chen, et al. Synergistic antitumor effect of brusatol combined with cisplatin on colorectal cancer cells. Int J Mol Med. 2018 Mar;41(3):1447-1454.

    [3]. Adedamola Olayanju, et al. Brusatol provokes a rapid and transient inhibition of Nrf2 signaling and sensitizes mammalian cells to chemical toxicity-implications for therapeutic targeting of Nrf2. Free Radic Biol Med. 2015 Jan;78:202-12.