Brusatol - CAS:14907-98-3

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Brusatol (Synonyms:鸦胆子苦醇; NSC 172924)

目录号 : KM11948 CAS No. : 14907-98-3 纯度 : 98%

Data Sheet 产品使用指南

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)。

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock

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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. Brusatol increases cellular apoptosis.

体外研究

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.
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.

Cell Viability Assay

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

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

"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.
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. "

Animal Model:	Athymic nude mice 4-6 wk old bearing A549 xenografts
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. "

分子式

C₂₆H₃₂O₁₁

分子量

520.53

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。
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。
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。

科研文献

纯度： 98%

Data Sheet

产品使用指南

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