CITCO

SKU: orb1218138

Description

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.

Key Properties

• CAS Number: 338404-52-7
• MW: 436.74
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₂Cl₃N₃OS
• SMILES: Clc(cc1)ccc1-c1c(/C=N/OCc(cc2)cc(Cl)c2Cl)n(ccs2)c2n1
• Target: CAR|PXR
• Solubility: DMSO:soluble; H2O:insoluble

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

CAR|PXR