Damnacanthal|cas:477-84-9|西域试剂

Damnacanthal,98.0%

产品编号：Bellancom-108485| CAS NO：477-84-9| 分子式：C₁₆H₁₀O₅| 分子量：282.25

Damnacanthal 是从 Morinda citrifolia 的根中分离出来的蒽醌。Damnacanthal 是一种强效选择性的 p56lck 酪氨酸激酶活性的抑制剂。天然的 Damnacanthal 抑制 p56lck 的自磷酸化和外源底物的磷酸化，IC50 分别为 46 nM 和 220 nM。Damnacanthal 是一种具有抗癌活性的有效凋亡诱导剂。Damnacanthal 在小鼠中也具有镇痛，抗炎作用，并且对白色念珠菌具有抗真菌活性。

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-108485		￥9800.00	杭州北京（现货）

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Damnacanthal

产品介绍

Damnacanthal 是从 Morinda citrifolia 的根中分离出来的蒽醌。Damnacanthal 是一种强效选择性的 p56^lck 酪氨酸激酶活性的抑制剂。天然的 Damnacanthal 抑制 p56^lck 的自磷酸化和外源底物的磷酸化，IC₅₀ 分别为 46 nM 和 220 nM。Damnacanthal 是一种具有抗癌活性的有效凋亡诱导剂。Damnacanthal 在小鼠中也具有抗炎作用，也可用于缓解疼痛的研究，并且对白色念珠菌具有抗真菌活性。

生物活性

Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56^lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 ^lck autophosphorylation and phosphorylation of exogenous substrates with IC₅₀s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans^[4].

体外研究

Damnacanthal has > 100-fold selectivity for p56^lck over the serine/threonine kinases, protein kinase A and protein kinase C, and > 40-fold selectivity for p56^lck over four receptor tyrosine kinases. Damnacanthal also demonstrates modest (7-20-fold), but highly statistically significant, selectivity for p56^lck over the homologous enzymes p60^src and p59^fyn.
Damnacanthal (0.1-100 μM; 1-4 days; HCT-116 and SW480 cells) treatment results in a significant reduction of cell proliferation in a concentration- and time-dependent manner.
Damnacanthal (1-50 μM; 72 hours; HCT-116 cells) treatment results in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM.
Damnacanthal (10 μM; 24 hours; HCT-116 cells) treatment significantly increases caspase 3/7 activity. Damnacanthal-induced apoptosis.
Damnacanthal (0.1-10 μM; 24 hours; HCT-116 cells) treatment induces NAG-1 expression in HCT-116 cells. Cyclin D1 expression is reduced at 10 μM of Damnacanthal, whereas p21 and p53 does not alter their expression. PARP cleavage is seen at 10 μM Damnacanthal treatment only in HCT-116 cells, where NAG-1 is induced.
Damnacanthal treatment for 2 weeks shows significant decreasing colony number in HCT-116 cells in a concentration-dependent manner. Damnacanthal-treated cells show a dramatic inhibition of clonogenic capacity. Damnacanthal-treated (1-50 μM; 48 hours) cells significantly inhibits the migration of HCT-116 cells in a concentration-dependent manner.

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

Cell Proliferation Assay

Cell Line:	HCT-116 and SW480 cells
Concentration:	0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time:	1, 2, and 4 days
Result:	Resulted in a significant reduction of cell proliferation in a concentration- and time-dependent manner.

Cell Cycle Analysis

Cell Line:	HCT-116 cells
Concentration:	1 μM, 10 μM and 50 μM
Incubation Time:	72 hours
Result:	Resulted in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM.

Apoptosis Analysis

Cell Line:	HCT-116 cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	Significantly increased caspase 3/7 activity.

Western Blot Analysis

Cell Line:	HCT-116 cells
Concentration:	0.1 μM, 1 μM and 10 μM
Incubation Time:	24 hours
Result:	NAG-1 was induced in HCT-116 cells in a dose- and time-dependent manner. Cyclin D1 expression was reduced at 10 μM.

体内研究
(In Vivo)

Damnacanthal (10-100 mg/kg; oral administration; for 10-300 minutes; male ddY mice) treatment exhibits a significant antinociceptive effect in a dose-dependent manner in the formalin test. Administration of damnacanthal (100 mg/kg) shows significant inhibition of histamine-induced paw edema^[4].

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

Animal Model:	Male ddY mice (5-6 weeks) injected with formalin or Histamine^[4]
Dosage:	10 mg/kg, 30 mg/kg and 100 mg/kg
Administration:	Oral administration; for 10 minutes, 30 minutes, 60 minutes or 300 minutes
Result:	Significantly reduced the growth of human lung tumor without acute toxicity.

体内研究

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

Animal Model:	Male ddY mice (5-6 weeks) injected with formalin or Histamine^[4]
Dosage:	10 mg/kg, 30 mg/kg and 100 mg/kg
Administration:	Oral administration; for 10 minutes, 30 minutes, 60 minutes or 300 minutes
Result:	Significantly reduced the growth of human lung tumor without acute toxicity.

体内研究

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

Animal Model:	Male ddY mice (5-6 weeks) injected with formalin or Histamine^[4]
Dosage:	10 mg/kg, 30 mg/kg and 100 mg/kg
Administration:	Oral administration; for 10 minutes, 30 minutes, 60 minutes or 300 minutes
Result:	Significantly reduced the growth of human lung tumor without acute toxicity.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (17.71 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5430 mL	17.7148 mL	35.4296 mL
5 mM	0.7086 mL	3.5430 mL	7.0859 mL
10 mM	0.3543 mL	1.7715 mL	3.5430 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： 0.5% CMC-Na/saline water
Solubility: 4 mg/mL (14.17 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 50% PEG300 50% saline
Solubility: 4 mg/mL (14.17 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在西域网站选购。

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)

参考文献

. Faltynek CR, et al. Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity. Biochemistry. 1995 Sep 26;34(38):12404-10. [Content Brief]

. Nualsanit T, et al. Damnacanthal, a noni component, exhibits antitumorigenic activity in human colorectal cancer cells. J Nutr Biochem. 2012 Aug;23(8):915-23. [Content Brief]

. Aziz MY, et al. Damnacanthal is a potent inducer of apoptosis with anticancer activity by stimulating p53 and p21 genes in MCF-7 breast cancer cells. Oncol Lett. 2014 May;7(5):1479-1484. [Content Brief]

[4]. Okusada K, et al. The antinociceptive and anti-inflammatory action of the CHCl3-soluble phase and its main active component, damnacanthal, isolated from the root of Morinda citrifolia. Biol Pharm Bull. 2011;34(1):103-7. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

1. 物质的识别

产品名：	Damnacanthal
CAS号：	477-84-9
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Damnacanthal
分子式：	C16H10O5
分子量：	282.25

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。