CITCO

Research use only, not for human use.

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 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 (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.

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.

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Others

Other Targets

CAR|PXR

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338404-52-7

436.74

C19H12Cl3N3OS

>98% (HPLC)

DMSO:soluble; H2O:insoluble

Clc(cc1)ccc1-c1c(/C=N/OCc(cc2)cc(Cl)c2Cl)n(ccs2)c2n1

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(-20℃)

With Ice Pack

≥ 2 years