中文名称: 鸦胆子苦醇
英文名称: Brusatol
CAS No: 14907-98-3
分子式: C26H32O11
分子量: 520.53
B10088 鸦胆子苦醇 ≥98%(HPLC) (psaitong)
包装规格:
20mg in glass bottle
溶解性:
溶于DMSO(5 mg/mL 加热)
产品描述:

基本信息

产品编号:

B10088

产品名称:

Brusatol

CAS:

14907-98-3

 

储存条件

粉末

-20℃

四年

分子式:

C26H32O11

溶于液体

-80℃

6个月

分子量:

520.53

-20℃

1个月

化学名: 

(1R,2S,3S,3aS,3a1R,4R,6aR,7aR,11aS,11bR)-Methyl

1,2,9-trihydroxy-8,11a-dimethyl-4-((3-methylbut-2-enoyl)oxy)-5,10-dioxo-2,3,3a,4,5,6a,7,7a,10,11,11a,11b-dodecahydro-1H-3,3a1-

Solubility (25°C):

 

体外:

 

DMSO

100mg/mL (192.11mM)

Ethanol

Insoluble

Water

Insoluble

体内(现配现用):

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% DMSO40% PEG3005% Tween-8045% saline

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

2. 请依序添加每种溶剂:10% DMSO90%(20% SBE-β-CD in saline)

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

3.请依序添加每种溶剂:10% DMSO90% corn oil

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

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

1.9211mL

9.6056mL

19.2112mL

5mM

0.3842mL

1.9211mL

3.8422mL

10mM

0.1921mL

0.9606mL

1.9211mL

 

生物活性

产品描述

一种来源于植物的天然类西林类药物,通过抑制细胞蛋白的从头合成,在肿瘤培养中表现出广泛的细胞毒性。

靶点

Nrf2

 

体外研究

Brusatol (0.05,0.15,0.45,1.35,4.05 and 12.15μg/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 Hepa1c1c7 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 12.15μg/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±0.01μg/mL.

Western Blot Analysis

Cell Line:

Mouse Hepa-1c1c7 hepatoma cells

Concentration:

1,3,10,30,100,300,and 1000nM

Incubation Time:

2 hours

Result:

Provoked the depletion of Nrf2,in a concentration-dependent manner within 2h 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 2mg/kg Brusatol.Nrf2 protein levels are significantly decreased at 24h or 48h postinjection.Cisplatin (2mg/kg) or Brusatol (2mg/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:

2mg/kg

Administration:

Treated i.p.;Cisplatin (2mg/kg),Brusatol (2mg/kg),or in combination every other day for a total of five times

Result:

Nrf2 protein levels were significantly decreased at 24h or 48h postinjection.Cisplatin or Brusatol alone did not inhibit tumor growth significantly, whereas in the combination group, tumor size was significantly reduced.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

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连续稀释计算器方程

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  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):