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CAS No.: 518-82-1

大黄素 Catalog No. CSN18468

Synonyms: 大黄素;Frangula emodin

Emodin shows antiproliferative effects in cancer cells that are regulated by different signaling pathways, it is a naturally occurring anthraquinone present in the roots and barks of numerous plants.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Lck

IC50:18.5μM
描述Among various Ser/Thr protein kinases, CKII plays a potential role in the processes of cell proliferation, transformation, and differentiation. In addition, abolition of CKII activity causes cell death in yeast, whereas overexpression of the CKII α-subunit gene in animal cells causes the cells to become oncogenic. Emodin, an anthraquinone derivative, selectively and competitively inhibits CKII with IC₅₀ of 2 μM and K_i of 7.2 μM^[5]. HepG2 cells treated with 25 μM emodin for 48 h displayed apoptotic morphological changes^[6]. Emodin killed T24 and J82 cells in a dose-dependent manner after 24 h treatment. It also killed T24 at concentration of 20 μM and J82 cells at concentration of 15 μM in a time-dependent manner. Mice treated with emodin and cisplatin had significantly smaller tumors than those from the other groups indicating emodin/cisplatin co-treatment can significantly suppress tumor growth in vivo^[7].

动物研究

剂量

Nude mice: 10 mg/kg - 80 mg/kg^[1] (i.p.) Wild type mice: 1 mg/kg^[2] (i.v.) Rat: 40 mg/kg, 80 mg/kg^[3] (p.o.)

给药途径

i.p., i.v., p.o.

动物药代数据

Animal	Rats^[4]
Dose	34.65 mg/kg
Administration	p.o.
V/F	1052 ± 119.8 L
T_1/2	23.13 ± 3.56 h
T_max	0.75 ± 0.00 h
C_max	91.65 ± 16.82 ng/ml
AUC_0→∞	1108 ± 191.1 ng·h/ml
MRT_0→∞	29.90 ± 4.71 h
CL/F	31.99 ± 5.15 L/h
AUC_0→t	624.7 ± 73.35 ng·h/ml

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00801268	Polycystic Kidney	Not Applicable	Terminated(high rate of drop-o... more >>ut) Collapse <<	-	China, Jiangsu ... more >> Liu ZH, Yao XD,Chen X,Hu YL Nanjing, Jiangsu, China, 210002 Yao Xiaodan Nanjing, Jiangsu, China, 210002 Collapse <<
NCT01287468	-	-	Unknown	December 2014	Taiwan ... more >> Taipei Medical University - WanFang Hospital Taipei, Taiwan Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7005 mL
- 18.5023 mL
- 37.0046 mL
- 5 mM
- 0.7401 mL
- 3.7005 mL
- 7.4009 mL
- 10 mM
- 0.3700 mL
- 1.8502 mL
- 3.7005 mL

技术信息

CAS号

518-82-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H10O5

运输

蓝冰

分子量

270.24

别名

大黄素;Frangula emodin

溶解度

DMSO	53.0 mg/mL (196.1 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (7.4 mM)

动物实验配方

8% DMSO+75% PEG 300+8% Tween 80+water

12 mg/mL

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