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  1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Chrysophanol

Chrysophanol  (Synonyms: 大黃酚; Chrysophanic acid)

目錄號(hào): HY-13595 純度: 99.77%
COA 產(chǎn)品使用指南 技術(shù)支持

Chrysophanol (Chrysophanic acid) 是一種天然蒽醌,抑制EGF-誘導(dǎo)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

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)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]
體外研究
(In Vitro)

Chrysophanol (Chrysophanic Acid) 通過抑制 EGFR/mTOR 通路來阻止結(jié)腸癌細(xì)胞的增殖。Chrysophanol 是一種天然蒽醌,在 EGFR 過表達(dá)的 SNU-C5 人結(jié)腸癌細(xì)胞中具有抗癌活性。SNU-C5 細(xì)胞中的 Chrysophanol 處理可抑制 EGF 誘導(dǎo)的 EGFR 磷酸化并抑制下游信號(hào)分子的激活,例如 AKT、細(xì)胞外信號(hào)調(diào)節(jié)激酶 (ERK) 和哺乳動(dòng)物雷帕霉素靶點(diǎn) (mTOR)/核糖體蛋白 S6 激酶 (p70S6K))。當(dāng)與 mTOR 抑制劑 Rapamycin 結(jié)合使用時(shí),Chrysophanol (80 和 120 μM) 顯著阻斷細(xì)胞增殖。Chrysophanol 抑制 EGF 誘導(dǎo)的 EGFR 磷酸化并抑制 AKT 和 mTOR/p70S6K 的激活,并顯著阻斷細(xì)胞增殖。Chrysophanol 劑量依賴性地降低 CCK-8 和 EGFR 過表達(dá) SNU-C5 細(xì)胞的活力。Chrysophanol 抑制劑量依賴性地降低 EGF 誘導(dǎo)的 EGFR Tyr1068 磷酸化。Chrysophanol (80 和 120 μM) 降低 mTOR 在 Ser2448 位點(diǎn)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 誘導(dǎo)的 EGFR 激活并抑制下游信號(hào)分子 AKT 和 mTOR/p70S6K 的激活[1]。Chrysophanol (CA) 抑制 3T3-L1 脂肪細(xì)胞中的脂質(zhì)積累。Chrysophanol 下調(diào) 3T3-L1 脂肪細(xì)胞中的脂肪生成因子。Chrysophanol 在原代培養(yǎng)的棕色脂肪細(xì)胞中誘導(dǎo)產(chǎn)熱因子。Chrysophanol 通過激活 AMPK 通路抑制脂肪生成并誘導(dǎo)產(chǎn)熱[2]。

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

體內(nèi)研究
(In Vivo)

Chrysophanol (CA) 可改善 C57BL/6 小鼠中 HFD 誘導(dǎo)的肥胖。Chrysophanol 的體內(nèi)性能在雄性 C57BL/6J 小鼠中進(jìn)行,以確定 Chrysophanol 給藥的功效。與喂食標(biāo)準(zhǔn)飲食的小鼠相比,喂食 HFD 的小鼠體重明顯增加。另一方面,Chrysophanol 組的體重增加明顯低于未處理的 HFD。HFD 組小鼠體重增加了 23.92 ± 1.74 g,而 Chrysophanol 組小鼠在 16 周后體重增加了 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 號(hào)
性狀

固體

顏色

Yellow to orange

中文名稱

大黃酚;大黃根酸

結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMF 中的溶解度 : 4 mg/mL (15.73 mM; 超聲助溶)

DMSO 中的溶解度 : 2 mg/mL (7.87 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.77%

參考文獻(xiàn)
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.

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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
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    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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產(chǎn)品名稱:
Chrysophanol
目錄號(hào):
HY-13595
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