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Acacetin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Acacetin图片
CAS NO:480-44-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
金合欢素
5,7-Dihydroxy-4'-methoxyflavone
产品介绍
Acacetin (5,7-Dihydroxy-4'-methoxyflavone) 是一种口服有效的类黄酮,来自Dendranthema morifolium。Acacetin 停在 PI3Kγ 的 ATP 结合口袋中。Acacetin 导致癌细胞周期停滞,并诱导细胞凋亡和自噬。Acacetin 具有有效的抗癌和抗炎活性,有用于疼痛相关疾病研究的潜力。
生物活性

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived fromDendranthema morifolium. Acacetin docks in the ATP binding pocket ofPI3Kγ. Acacetin causes cell cycle arrest and inducesapoptosisandautophagyincancercells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research[1][2].

体外研究
(In Vitro)

Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 10-200 μM; 24 hours) decreases cell viabilities in a dose-dependent manner. Acacetin has little effect on human normal glial cell line HEB and non-tumorigenic epithelial cell line MCF-10A[1].
Acacetin (50-150 μM; 24 hours) causes G2/M cell cycle arrest and induces apoptosis and autophagy[1].
Acacetin (50-150 μM; 24 hours) leads to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner[1].

Cell Viability Assay[1]

Cell Line:Breast cancer MCF-7 cells, hepatocellular carcinoma SMMC-7721 cells, lung adenocarcinoma A549 cells, esophageal carcinoma Eca109 cells
Concentration:10, 20, 40, 60, 80, 100, 150, 200 μM
Incubation Time:24 hours
Result:Decreased cancer cell viabilities in a dose-dependent manner.
Had IC50values of 82.75 μM, 103.9 μM, 157.4 μM, 54.7 μM in MDA-MB-231, MCF-7, A549, Eca109 cells, respectively.

Cell Cycle Analysis[1]

Cell Line:MDA-MB-231 cells
Concentration:50, 100, 150 μM
Incubation Time:24 hours
Result:Resulted in increase in percentage of cells at G2/M phase and decrease in percentage of cells at G1 and S phase in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line:MDA-MB-231 cells
Concentration:50, 100, 150 μM
Incubation Time:24 hours
Result:Induced apoptosis.

Cell Autophagy Assay[1]

Cell Line:MDA-MB-231 cells
Concentration:50, 100, 150 μM
Incubation Time:24 hours
Result:Induced autophagy.
Resulted in marked increases in EGFP-LC3 puncta formation and a dose-dependent accumulation of LC3-II.

Western Blot Analysis[1]

Cell Line:MDA-MB-231 cells
Concentration:50, 100, 150 μM
Incubation Time:24 hours
Result:Resulted in decrease in levels of Bcl-2 and Bcl-xL and increase in levels of p53.
Led to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner.
Had little or no effect on expression of PI3Kα, PI3Kβ, PI3Kδ, p-ERK, p-p38, and p-JNK.
体内研究
(In Vivo)

Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 5, 20 mg/kg/day; orally; for 3 days) significantly suppresses microglial activation in an LPS-induced neuroinflammation mouse model[2].
Acacetin (25 mg/kg/day; orally; for 3 days) reduces neuronal cell death in an animal model of ischemia[2].
Acacetin (1.8-56.2 mg/kg/day; ip; single dose) decreases visceral and inflammatory nociception and prevented the formalin-induced oedema[3].

Animal Model:Male C57BL/6 mice, 7 weeks of age[2]
Dosage:5, 20 mg/kg
Administration:Orally; once a day for 3 days
Result:Significantly suppressed microglial activation in an LPS-induced (ip; 5mg/kg) neuroinflammation mouse model.
分子量

284.26

性状

Solid

Formula

C16H12O5

CAS 号

480-44-4

中文名称

金合欢素;刺槐黄素

结构分类
  • Flavonoids
  • Flavones
  • Phenols
  • Polyphenols
来源
  • Plants
  • Leguminosae
  • Melilotus albusMedic. ex Desr
  • Plants
  • Compositae
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL(439.74 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.5179 mL17.5895 mL35.1791 mL
5 mM0.7036 mL3.5179 mL7.0358 mL
10 mM0.3518 mL1.7590 mL3.5179 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: 0.5%CMC-Na/saline water

    Solubility: 10 mg/mL (35.18 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 50%PEG300   50% saline

    Solubility: 5 mg/mL (17.59 mM); Suspended solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂: 0.5% CMC/saline water

    Solubility: 2.5 mg/mL (8.79 mM); Suspended solution; Need ultrasonic

  • 4.

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

    Solubility: ≥ 2.08 mg/mL (7.32 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.32 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 20.8 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本网站选购。