Tryptanthrin
(Synonyms: 色胺酮,NSC 349447) 目录号 : GC13402An alkaloid with diverse actions
Cas No.:13220-57-0
Sample solution is provided at 25 µL, 10mM.
Tryptanthrin, a weakly basic alkaloid tryptophan derivative originally isolated from the dried roots of medicinal indigo plants, has anti-inflammatory and anticancer activities. And, tryptanthrin blocks 5-lipoxygenase (5-LO) and cyclooxygenase-2 (Cox-2) with IC50 values of 600 and 64 nM, respectively.
5-LO and Cox-2 are involved in cancer pathobiology. 5-LO is expressed by a variety of cancer cells including colon, lung, breast, and prostate and promotes cancer cell growth and neo-angiogenesis. Cox-2, overexpressed in cancer cells, promotes tumorigenesis and induces neo-angiogenesis.
In vitro: In human hepatocyte-derived HepG2 cells, tryptanthrin inhibited the reactive oxygen species formation, mitochondrial dysfunction, and cell death triggered by tert-butyl hydroperoxide (tBHP). Furthermore, tryptanthrin reversed the reduction of glutathione (GSH) induced by tBHP. Specifically, nuclear translocation, transactivation of nuclear factor erythroid 2-related factor 2 (Nrf2), and phosphorylation of extracellular signal-regulated kinase (ERK) were evoked by the treatment of tryptanthrin. Additionally, the expression of the heme oxygenase 1 and glutamate was upregulated by tryptanthrin [1].
In vivo: BALB/c (H-2d) mice, intraperitoneally (i.p.) inoculated with leukemia WEHI-3B JCS cells, were injected i.p with tryptanthrin at doses of 0.04 mg/kg, 0.08 mg/kg and 0.16 mg/kg body weight for 5 consecutive days. Tryptanthrin inhibited the growth of WEHI-3B JCS cells in BALB/c mice, and at the dosages of 0.08 mg/kg and 0.16 mg/kg, significant inhibition was seen. Moreover, tryptanthrin, in a dose-dependent fashion, triggered cell cycle arrest of the WEHI-3B JCS cells at G0/G1 phase [2].
References:
[1]. Moon, S., Lee, J., Choi, H., Cho, I., Kim, S., & Kim, Y. Tryptanthrin Protects Hepatocytes against Oxidative Stress via Activation of the Extracellular Signal-Regulated Kinase/NF-E2-Related Factor 2 Pathway. Biological and Pharmaceutical Bulletin. 2014; 37(10): 1633-1640.
[2]. Chan, H., Yip, H., Mak, N., & Leung, K. Modulatory Effects and Action Mechanisms of Tryptanthrin on Murine Myeloid Leukemia Cells. Cellular and Molecular Immunology. 2009; 6(5): 335-342.
Cas No. | 13220-57-0 | SDF | |
别名 | 色胺酮,NSC 349447 | ||
化学名 | indolo[2,1-b]quinazoline-6,12-dione | ||
Canonical SMILES | O=C1N2C(C(C3=C2C=CC=C3)=O)=NC4=C1C=CC=C4 | ||
分子式 | C15H8N2O2 | 分子量 | 248.2 |
溶解度 | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.029 mL | 20.145 mL | 40.2901 mL |
5 mM | 0.8058 mL | 4.029 mL | 8.058 mL |
10 mM | 0.4029 mL | 2.0145 mL | 4.029 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet