Xanthatin - CAS:26791-73-1

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Xanthatin (Synonyms:苍耳亭)

目录号 : KM14490 CAS No. : 26791-73-1 纯度 : 98%

Data Sheet 产品使用指南

Xanthatin 从 Xanthium strumarium 叶子中提取，诱导细胞凋亡 (apoptosis)。Xanthatin 通过抑制 PGE2 的合成和 5-脂氧合酶的活性而显示出抗炎活性。Xanthatin 抑制布鲁氏菌的 IC₅₀ 值为 2.63 μg/ mL，对寄生虫特异性锥虫硫磷还原酶具有不可逆的弱抑制作用。

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10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC₅₀ of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer.

体外研究

Xanthatin is against T. b. brucei with an IC₅₀ value of 2.63 µg/mL and exhibits weak irreversible inhibition of parasite specific trypanothione reductase.
Xanthatin (0-40 μM; 24 hours) has obscure inhibition effect on the proliferation of HUVEC in the absence of VEGF.
Xanthatin (5-40 μM; 24 hours) inhibits breast cancer cell proliferation in a dose responsive manner. Xanthatin inhibits HCC1937, MDA-MB-415, SK-BR-3, MCF-7 and MDA-MB-231 with IC₅₀ values of 81 μM, 31 μM, 38 μM, 30 μM, and 17 μM, respectively.
Xanthatin (0-10 μM; 24 hours) dose dependently suppresses the phosphorylation of STAT3 (Ser727), at the same time, it also results in a rapid dephosphorylation of down-stream kinases of STAT3, including PI3K and Akt, including PI3K (p-PI3K p85 _tyr458) and Akt.

Cell Proliferation Assay

Cell Line:	HUVEC cells
Concentration:	0 μM, 5 μM, 10 μM, 15 μM, 20 μM, 30 μM, 40 μM
Incubation Time:	24 hours
Result:	Inhibited cell growth from dose 10 μM in the presence of vEGF.

Cell Viability Assay

Cell Line:	HCC1937, MDA-MB-415, SK-BR-3, MCF-7 and MDA-MB-231 cells
Concentration:	5, 10, 15, 20, 30, and 40 μM
Incubation Time:	24 hours
Result:	Inhibited breast cancer cell growth.

Western Blot Analysis

Cell Line:	HUVEC cells
Concentration:	0, 3, and 10 μM
Incubation Time:	24 hours
Result:	Inhibited VEGFR2 downstream signaling pathways and blocked VEGF-induced STAT3 activation in HUVEC.

体内研究

Xanthatin (intragastric administration; 20 mg/kg; once daily; 25 days) leads to significant inhibition of tumor volume. And this compound is well-tolerated and exhibits no significant difference in weight compares to the vehicle group.

Animal Model:	Transplanted MDA-MB-231 cells into mice and constucted human breast cancer xenograft mouse model
Dosage:	20 mg/kg; once daily; 25 days
Administration:	Intragastric administration
Result:	Supressed tumor growth and tumor angiogenesis in vivo.

分子式

C₁₅H₁₈O₃

分子量

246.30

CAS号

26791-73-1

中文名称

苍耳亭

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (406.01 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.0601 mL	20.3004 mL	40.6009 mL
5 mM	0.8120 mL	4.0601 mL	8.1202 mL
10 mM	0.4060 mL	2.0300 mL	4.0601 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 (protect from light)。-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: ≥ 4.55 mg/mL (18.47 mM); Clear solution

此方案可获得 ≥ 4.55 mg/mL (18.47 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 45.5 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 (10.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.15 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 (10.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.15 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。