1. Apoptosis
  2. Apoptosis
  3. CITCO

CITCO 

Cat. No.: HY-103244
Handling Instructions

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.

For research use only. We do not sell to patients.

CITCO Chemical Structure

CITCO Chemical Structure

CAS No. : 338404-52-7

Size Stock
1 mg   Get quote  
5 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

IC50 & Target

CAR, PXR[1]

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.
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.
Molecular Weight

436.74

Formula

C₁₉H₁₂Cl₃N₃OS

CAS No.

338404-52-7

SMILES

ClC1=CC=C(C2=C(/C=N/OCC3=CC=C(Cl)C(Cl)=C3)N4C(SC=C4)=N2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CITCO
Cat. No.:
HY-103244
Quantity: