| 產(chǎn)品描述： | CITCO 是一種組成型雄甾烷受體(constitutive androstane receptor)激動劑，其EC50 為 49 nM。CITCO 在瞬時轉(zhuǎn)染試驗中對 CAR 的選擇性比 PXR 高 50 倍 |
| 靶點： |
CAR(in CAR/SRC-1 FRET assay):49 nM(EC50);Apoptosis |
| 體外研究： |
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 |
| 體內(nèi)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. |
| 細胞實驗： |
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 |
| 動物實驗： |
Animal Models: Six- to eight-week-old male athymic nude mice Dosages: 25 μg, 100?μg Administration: i.v. |
| 參考文獻： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京