CITCO 是一种咪唑噻唑衍生物，也是一种选择性组成型雄甾烷受体激动剂。它抑制脑肿瘤干细胞的生长和扩增，其 EC50 比孕烷 X 受体为 49?nM

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. CITCO is an imidazothiazole derivative and it also is a selective Constitutive androstane receptor (CAR) agonist.

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

CITCO (intraperitoneal; 25?μg; on days 22, 24, 26, 30 and 36) results a significant decrease in tumour growth. After treatment with 100?μg CITCO, it further decreases to an undetectable level [1].

338404-52-7

C19H12Cl3N3OS

436.74

DMSO:11 mg/ml (25.19 mM)
H2O:insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years