CITCO

An agonist of human CAR

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5mg

￥775.00

620.00

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10mg

￥1225.00

980.00

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25mg

￥2237.00

1790.00

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Background

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[1].

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[1]. CITCO (2.5, 5?μM; 48?hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes[1]. CITCO (2.5-10?μM; 48?hours) induces apoptosis in BTSCs in culture in dose dependently, but not in normal astrocytes[1]. CITCO (0-25?μM; 48?hours) causes the T98G and U87MG glioma and BTSCs expressing very low levels of CAR protein that increased significantly[1].

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 [1].

参考文献:
[1]. 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.