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CITCO

Catalog No.
B7468
A selective constitutive androstane receptor (CAR) agonist
Grouped product items
SizePriceStock Qty
5mg
$81.00
In stock
10mg
$152.00
In stock
25mg
$342.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

CITCO, an imidazothiazole derivative, is a selective agonist of human CAR, with an EC50 value of 49 nM and > 50-fold selectivity to CAR over pregnane X receptor (PXR), and no activity on other nuclear receptors. Upon activation with specific agonists, CAR translocates into the nucleus and binds to the response elements as monomers or CAR/RXR heterodimers. The CAR functions as a xenobiotic receptor, involved in detoxification and clearance of toxic substances from the liver. In addition, activation with selective CAR agonists such as CITCO has also been shown to inhibit growth and expansion of brain tumor stem cells. 

Reference:

1. Chakraborty S, Kanakasabai S, Bright JJ. Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. British Journal of Cancer, 2011, 104(3): 448-459.

Product Citation

Chemical Properties

Physical AppearanceA crystalline solid
StorageDesiccate at -20°C
M.Wt436.74
Cas No.338404-52-7
FormulaC19H12Cl3N3OS
SolubilitySoluble in DMSO
Chemical Name(E)-6-(4-chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime
SDFDownload SDF
Canonical SMILESClC1=CC=C(C=C1)C2=C(/C=N/OCC(C=C3Cl)=CC=C3Cl)N4C(SC=C4)=N2
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment:[1]

Cell lines

T98G, U87MG, DB29 and DB33 glioma cells

Reaction Conditions

2.5 ~ 10 μM CITCO for 48 h incubation

Applications

The brain tumor stem cells (BTSCs) from T98G and U87MG cultured in the absence of CITCO showed 6.8 and 11% Annexin V-positive cells that increased to 62 and 68% following addition of 10 μM CITCO, respectively. Moreover, BTSCs from DB29 and DB33 gliomas showed 3 and 0.5% Annexin V-positive cells that increased to 24 and 41% following treatment with 10 μM CITCO, respectively. CITCO dose-dependently induced apoptosis in BTSCs in culture, but not in normal astrocytes.

Animal experiment:[1]

Animal models

Nude mice subcutaneously injected with U87MG–BTSCs

Dosage form

25 or 100 μg

Intraperitoneal injection; on days 22, 24, 26, 30 and 36

Applications

CITCO at the dose of 25 μg resulted in a significant decrease in tumour growth, which further decreased to an undetectable level after treatment with 100 μg CITCO.

Note

The technical data provided above is for reference only.

References:

1. Chakraborty S, Kanakasabai S, Bright JJ. Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. British Journal of Cancer, 2011, 104(3): 448-459.

Quality Control

Quality Control & MSDS

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Chemical structure

CITCO

Related Biological Data

CITCO

Related Biological Data

CITCO