CITCO
- CAS号:338404-52-7
- 英文名:CITCO
- 中文名:CITCO
- CBNumber:CB4497318
- 分子式:C19H12Cl3N3OS
- 分子量:436.74
- MOL File:338404-52-7.mol
- 密度 :1.48±0.1 g/cm3(Predicted)
- 储存条件 :-20°C
- 溶解度 :DMSO: 28 mg/mL, soluble
- 形态 :solid
- 酸度系数(pKa) :4.05±0.40(Predicted)
- 颜色 :Light yellow to yellow
CITCO性质、用途与生产工艺
- 生物活性 CITCO 是一种组成型雄甾烷 (Constitutive androstane) 受体激动剂，抑制脑肿瘤干细胞 (BTSCs) 的生长和扩增。CITCO 是一种咪唑并噻唑衍生物，其作为人 CAR 的选择性激动剂起作用。CITCO 对于孕烷 X 受体 (PXR) 的 EC50 为 49 nM，并且对其他核受体没有活性。
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靶点
CAR, PXR
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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 that increased significantly.Cell Proliferation Assay
Cell Line: T98G, U87MG, DB29 and DB33 human glioma cells, astrocytes Concentration: 1, 2.5, 5, 10, 25, 50 μM Incubation Time: 48 hours Result: Resulted in a dose-dependent inhibition of viable cell count and proliferation. Cell Cycle Analysis
Cell Line: The T98G, U87MG, DB29 and DB33 glioma cells Concentration: 2.5, 5 μM Incubation Time: 48 hours Result: Induced cell cycle arrest differentially in different BTSCs in culture. Apoptosis Analysis
Cell Line: The T98G, U87MG, DB29 and DB33 glioma cells Concentration: 2.5, 5 or 10 μM Incubation Time: 48 hours Result: Increased the levels of Annexin V-positive apoptotic cells in dose dependently. Western Blot Analysis
Cell Line: T98G, U87MG, DB29 and DB33 glioma cells Concentration: 0 to 25 μM Incubation Time: 48 hours Result: The T98G, U87MG glioma and BTSCs expressed very low levels of CAR protein that increased significantly. -
体内研究
CITCO (intraperitoneal; on days 22, 24, 26, 30 and 36) with 25 μg results a significant decrease in tumour growth, which further decreases to an undetectable level after treatment with 100 μg CITCO .
Animal Model: Six- to eight-week-old male athymic nude mice Dosage: 25 or 100 μg Administration: Intraperitoneal; on days 22, 24, 26, 30 and 36 Result: Decreased tumour growth.
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