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CITCO

  Cat. No.:  DC32532   Featured
Chemical Structure
338404-52-7
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More than 5000 active chemicals with high quality for research!
Field of application
CITCO is a potent constitutive androstane receptor (CAR) agonist (EC50 = 49 nM). CITCO altered expression of key drug-metabolizing enzymes and transporters in human hepatocytes, which positively affects the metabolic profile of CHOP. Coadministration of CITCO and CHOP in the coculture model led to significantly enhanced cytotoxicity in lymphoma cells but not in cardiomyocytes. Constitutive androstane receptor (Car)-driven regeneration protects liver from failure following tissue loss. The constitutive androstane receptor (CAR and NR1i3) is a key regulator of CYP2B6.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 338404-52-7
Chemical Name: (E)-6-(4-chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime
Synonyms: CITCO
SMILES: ClC1=CC=C(C=C1Cl)CO/N=C/C2=C(C3=CC=C(Cl)C=C3)N=C4SC=CN42
Formula: C19H12Cl3N3Os
M.Wt: 436.735
Purity: >98%
Sotrage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Description: 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].
Target: CAR, PXR[1]
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 [1]. Animal Model: Six- to eight-week-old male athymic nude mice[1] 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[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]. Cell Proliferation Assay[1] 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[1] 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[1] 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[1] 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.
References: [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.
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