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  2. EGFR
  3. Chrysophanol

Chrysophanol  (Synonyms: 大黄酚; Chrysophanic acid)

目录号: HY-13595 纯度: 99.77%
COA 产品使用指南

Chrysophanol (Chrysophanic acid) 是一种天然蒽醌,抑制EGF-诱导的 EGFR 磷酸化,且抑制 AKTmTOR/p70S6K 激活。

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Chrysophanol Chemical Structure

Chrysophanol Chemical Structure

CAS No. : 481-74-3

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Other Forms of Chrysophanol:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.

IC50 & Target[1]

EGFR

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
5.7 μM
Compound: 26
Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by sulforhodamine B assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by sulforhodamine B assay
[PMID: 33691166]
Calu-1 IC50
> 100 μM
Compound: 6
Inhibition of human Calu1 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human Calu1 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
HCT-116 IC50
47.4 μM
Compound: 1
Cytotoxicity against MDR1 Pgp under-expressing human HCT116 cells after 24 hrs by MTT assay
Cytotoxicity against MDR1 Pgp under-expressing human HCT116 cells after 24 hrs by MTT assay
[PMID: 17949858]
HeLa IC50
> 100 μM
Compound: 6
Inhibition of human HeLa cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human HeLa cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
HepG2 IC50
64.4 μM
Compound: 1
Cytotoxicity against MDR1 Pgp overexpressing human HepG2 cells after 24 hrs by MTT assay
Cytotoxicity against MDR1 Pgp overexpressing human HepG2 cells after 24 hrs by MTT assay
[PMID: 17949858]
K562 IC50
> 100 μM
Compound: 6
Inhibition of human K562 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human K562 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
NCI-H157 IC50
2.7 μM
Compound: 26
Antiproliferative activity against human NCI-H157 cells assessed as reduction in cell viability measured after 72 hrs by sulforhodamine B assay
Antiproliferative activity against human NCI-H157 cells assessed as reduction in cell viability measured after 72 hrs by sulforhodamine B assay
[PMID: 33691166]
Raji IC50
> 100 μM
Compound: 6
Inhibition of human Raji cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human Raji cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
Vero IC50
> 100 μM
Compound: 6
Inhibition of african green monkey Vero cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of african green monkey Vero cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
WISH IC50
> 100 μM
Compound: 6
Inhibition of human WISH cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
Inhibition of human WISH cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting
[PMID: 11374975]
体外研究
(In Vitro)

Chrysophanol (Chrysophanic Acid) 通过抑制 EGFR/mTOR 通路来阻止结肠癌细胞的增殖。Chrysophanol 是一种天然蒽醌,在 EGFR 过表达的 SNU-C5 人结肠癌细胞中具有抗癌活性。SNU-C5 细胞中的 Chrysophanol 处理可抑制 EGF 诱导的 EGFR 磷酸化并抑制下游信号分子的激活,例如 AKT、细胞外信号调节激酶 (ERK) 和哺乳动物雷帕霉素靶点 (mTOR)/核糖体蛋白 S6 激酶 (p70S6K))。当与 mTOR 抑制剂 Rapamycin 结合使用时,Chrysophanol (80 和 120 μM) 显著阻断细胞增殖。Chrysophanol 抑制 EGF 诱导的 EGFR 磷酸化并抑制 AKT 和 mTOR/p70S6K 的激活,并显著阻断细胞增殖。Chrysophanol 剂量依赖性地降低 CCK-8 和 EGFR 过表达 SNU-C5 细胞的活力。Chrysophanol 抑制剂量依赖性地降低 EGF 诱导的 EGFR Tyr1068 磷酸化。Chrysophanol (80 和 120 μM) 降低 mTOR 在 Ser2448 位点的磷酸化水平。Chrysophanol (80 和 120 μM) 也降低 p70S6K 在 Thr389 的磷酸化水平。Chrysophanol 抑制 EGF 诱导的 EGFR 激活并抑制下游信号分子 AKT 和 mTOR/p70S6K 的激活[1]。Chrysophanol (CA) 抑制 3T3-L1 脂肪细胞中的脂质积累。Chrysophanol 下调 3T3-L1 脂肪细胞中的脂肪生成因子。Chrysophanol 在原代培养的棕色脂肪细胞中诱导产热因子。Chrysophanol 通过激活 AMPK 通路抑制脂肪生成并诱导产热[2]

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

体内研究
(In Vivo)

Chrysophanol (CA) 可改善 C57BL/6 小鼠中 HFD 诱导的肥胖。Chrysophanol 的体内性能在雄性 C57BL/6J 小鼠中进行,以确定 Chrysophanol 给药的功效。与喂食标准饮食的小鼠相比,喂食 HFD 的小鼠体重明显增加。另一方面,Chrysophanol 组的体重增加明显低于未处理的 HFD。HFD 组小鼠体重增加了 23.92 ± 1.74 g,而 Chrysophanol 组小鼠在 16 周后体重增加了 16.72 ± 2 g[2]

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

分子量

254.24

Formula

C15H10O4

CAS 号
性状

固体

颜色

Yellow to orange

中文名称

大黄酚;大黄根酸

结构分类
初始来源
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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMF 中的溶解度 : 4 mg/mL (15.73 mM; 超声助溶)

DMSO 中的溶解度 : 2 mg/mL (7.87 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9333 mL 19.6665 mL 39.3329 mL
5 mM 0.7867 mL 3.9333 mL 7.8666 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.77%

参考文献
Cell Assay
[1]

The cells are seeded at 5×103 cells/mL in 96-well microplates and allowed to attach for 24 h. Chrysophanol (20, 50, 80 and 120 μM) is added to the medium at various concentrations up to 120 μM and for different durations. After treatment, cell cytotoxicity and/or proliferation is assessed by a Cell Counting Kit-8 (CCK-8). Briefly, highly water-soluble tetrazolium salt, WST-8, produces an orange colored water-soluble product, formazan. The amount of formazan dye generated by dehydrogenases in cells is directly proportional to the number of living cells.CCK-8 (10 μL) is added to each well and incubated for 3 h at 37°C, then cell proliferation and cytotoxicity are assessed by measuring the absorbance at 450 nm using a microplate reader.Three replicated wells are used for each experimental condition[1].

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

Animal Administration
[2]

Mice[2]
Male 4-week-old C57BL/6J mice are maintained for 1 week prior to experiments. Mice are maintained on a 12-h light/dark cycle in a pathogen-free animal facility, provided with laboratory diet and water ad libitum. To induce obesity, the mice are fed a HFD with 60% kcal% fat. Control group (C) are fed a commercial standard chow diet. HFD group (HFD) mice are fed with HFD only. HFD plus CA group (CA) Mice are fed with HFD for 4 weeks before administration of Chrysophanol (5 mg/kg/day). The mice are divided into three groups (n = 5) that are fed chow diet, HFD, and HFD plus Chrysophanol for 16 weeks. Body weight and food intake are measured three times per week.

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

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / DMF 1 mM 3.9333 mL 19.6665 mL 39.3329 mL 98.3323 mL
5 mM 0.7867 mL 3.9333 mL 7.8666 mL 19.6665 mL
DMF 10 mM 0.3933 mL 1.9666 mL 3.9333 mL 9.8332 mL
15 mM 0.2622 mL 1.3111 mL 2.6222 mL 6.5555 mL
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.

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产品名称:
Chrysophanol
目录号:
HY-13595
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