Alantolactone - CAS:546-43-0

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Alantolactone (Synonyms:土木香内酯; (+-Alantolactone; Alant camphor; Inula camphor))

目录号 : KM12229 CAS No. : 546-43-0 纯度 : 98%

Alantolactone 是 STAT3 的选择性抑制剂，并具有抗肿瘤活性。Alantolactone 可诱导癌症相关的凋亡。

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生物活性

Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone induces apoptosis in cancer.

体外研究

Alantolactone induces apoptosis in HepG2 cells in a dose-dependent manner. This Alantolactone-induced apoptosis is found to be associated with GSH depletion, inhibition of STAT3 activation, ROS generation, mitochondrial transmembrane potential dissipation, and increased Bax/Bcl-2 ratio and caspase-3 activation. Alantolactone decreases STAT3 translocation to the nucleus, its DNA-binding, and STAT3 target gene expression. Alantolactone significantly inhibits STAT3 activation with a marginal effect on MAPKs and on NF-κB transcription; however, this effect is not mediated by inhibiting STAT3 upstream kinases.
Alantolactone induces activin/SMAD3 signaling in human colon adenocarcinoma HCT-8 cells. Alantolactone performs its antitumor effect by interrupting the interaction between Cripto-1 and the activin receptor type IIA in the activin signaling pathway.
Alantolactone (5 μg/mL, 24 h) inhibits cell proliferation in colon adenocarcinoma HCT-8 cells.

Cell Viability Assay

Cell Line:	HCT-8 cells.
Concentration:	5 μg/mL (~21.6 μM).
Incubation Time:	24 h.
Result:	Activated the activin signaling pathway in HCT-8 cells.

体内研究

It is found that the average tumor volume in the Alantolactone-treated mice is approximately 2.17-fold lower compared with that in the control mice. However the administration of Alantolactone does not affect the overall bodyweight during the experimental period, suggesting no apparent toxicity. Additionally, the average tumor weight is significantly lower in the Alantolactone-treated mice compared with the control mice. What’s more, the administration of Alantolactone results in a significant decrease in p-STAT3 and cyclin D1 expression in the tumor tissues.

Animal Model:	Female athymic BALB/c nude mice at the age of 6 weeks.
Dosage:	2.5 mg/kg.
Administration:	I.P. injection every 2 days.
Result:	Exhibited anti-cancer activity.

分子式

C₁₅H₂₀O₂

分子量

232.32

CAS号

546-43-0

中文名称

土木香内酯；木香腦；土木香脑；阿兰内酯；木香油內酯

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 : ≥ 100 mg/mL (430.44 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.3044 mL	21.5220 mL	43.0441 mL
5 mM	0.8609 mL	4.3044 mL	8.6088 mL
10 mM	0.4304 mL	2.1522 mL	4.3044 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.76 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.76 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.76 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

科研文献

纯度： 98%

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