CITCO

CITCO is a potent and selective constitutive androstane receptor (CAR) agonist with EC50 of 49 nM. CITCO displays >50-fold selectivity for CAR over PXR in the transient transfection assay.

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.^{<a class="sref" href="#s_ref">[2]</a>}

CITCO with 25 μg results a significant decrease in tumour growth, which further decreases to an undetectable level after treatment with 100 μg CITCO. ^{<a class="sref" href="#s_ref">[2]</a>}

• 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.

• Animal Models

  Six- to eight-week-old male athymic nude mice

• Dosages

  25 μg, 100 μg

• Administration

  i.v.