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编 号:F325525
分子式:C19H12Cl3N3OS
分子量:436.74
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49?nM over pregnane X receptor (PXR), and no activity on other nuclear receptors.

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.

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.
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