| 产品描述： | CITCO 是一种组成型雄甾烷受体(constitutive androstane receptor)激动剂，其EC50 为 49 nM。CITCO 在瞬时转染试验中对 CAR 的选择性比 PXR 高 50 倍 |
| 靶点： |
CAR(in CAR/SRC-1 FRET assay):49 nM(EC50);Apoptosis |
| 体外研究： |
CITCO (1-50 μM; 48 hours) results in a dose-dependent inhibition of viable cell count and proliferation in both T98G and U87MG glioma and BTSCs. CITCO (2.5, 5 μM; 48 hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes. CITCO (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in culture in dose dependently, but not in normal astrocytes. CITCO (0-25 μM; 48 hours) causes the T98G and U87MG glioma and BTSCs expressing very low levels of CAR protein |
| 体内研究： |
CITCO with 25 μg results a significant decrease in tumour growth, which further decreases to an undetectable level after treatment with 100 μg CITCO. |
| 细胞实验： |
Cell lines: Human glioma cell lines, primary human astrocytes Concentrations: 1, 2.5, 5, 10, 25, 50 μM Incubation Time: 48 h Method: The glioma cells are dissociated using 0.25% trypsin with 0.05 mM EDTA solution and subcultured once in 3–5 days. Primary human astrocytes are cultured in astrocyte medium.Cells are cultured in the absence or presence of CITCO at 37°C for different time points for proliferation assay, cell cycle analysis, apoptosis assay |
| 动物实验： |
Animal Models: Six- to eight-week-old male athymic nude mice Dosages: 25 μg, 100 μg Administration: i.v. |
| 参考文献： |
1. Jodi M Maglich, et al. Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes. J Biol Chem. 2003 May 9;278(19):17277-83. 2. Chakraborty S, et al. Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. Br J Cancer. 2011 Feb 1;104(3):448-59. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.29 ml |
11.448 ml |
22.896 ml |
| 5 mM |
0.458 ml |
2.29 ml |
4.579 ml |
| 10 mM |
0.229 ml |
1.145 ml |
2.29 ml |
| 50 mM |
0.046 ml |
0.229 ml |
0.458 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京