Acacetin

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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。

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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	3.5179 mL	17.5895 mL	35.1791 mL
5 mM	0.7036 mL	3.5179 mL	7.0358 mL
10 mM	0.3518 mL	1.7590 mL	3.5179 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。