| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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CITCO is an imidazothiazole-based constitutive androstane receptor (CAR) agonist (EC50 = 49 nM) with potential anticancer activity. It inhibits the growth of brain tumour stem cells (BTSCs)
| Targets |
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|---|---|---|
| ln Vitro |
In T98G and U87MG gliomas as well as BTSCs, CITCO (1-50 μM; 48 hours) causes a dose-dependent suppression of viable cell count and proliferation[1]. Different BTSCs in culture experience cell cycle arrest in different ways when exposed to CITCO (2.5, 5 μM) for 48 hours, while normal astrocytes are not affected[1]. In BTSCs in vitro, CITCO (2.5-10 μM; 48 hours) dose-dependently promotes apoptosis, but not in normal astrocytes[1]. T98G and U87MG gliomas, as well as BTSCs expressing extremely low quantities of CAR protein that rapidly increased, are caused by CITCO (0-25 μM; 48 hours)[1].
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| ln Vivo |
Treatment with 25 μg of CITCO (intraperitoneal; on days 22, 24, 26, 30, and 36) significantly reduces tumor development, and treatment with 100 μg of CITCO further reduces tumor growth to an undetectable level [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: T98G, U87MG, DB29 and DB33 human glioma cells, astrocytes Tested Concentrations: 1, 2.5, 5, 10, 25, 50 μM Incubation Duration: 48 hrs (hours) Experimental Results: Resulted in a dose-dependent inhibition of viable cell count and proliferation. Cell Cycle Analysis[1] Cell Types: The T98G, U87MG, DB29 and DB33 glioma cells Tested Concentrations: 2.5, 5 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced cell cycle arrest differentially in different BTSCs in culture. Apoptosis Analysis[1] Cell Types: The T98G, U87MG, DB29 and DB33 glioma cells Tested Concentrations: 2.5, 5 or 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: Increased the levels of Annexin V-positive apoptotic cells in dose dependently. Western Blot Analysis[1] Cell Types: T98G, U87MG, DB29 and DB33 glioma cells Tested Concentrations: 0 to 25 μM Incubation Duration: 48 hrs (hours) Experimental Results: The T98G, U87MG glioma and BTSCs expressed very low levels of CAR protein that increased Dramatically. |
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| Animal Protocol |
Animal/Disease Models: Six- to eightweeks old male athymic nude mice[1]
Doses: 25 or 100 μg Route of Administration: Intraperitoneal; on days 22, 24, 26, 30 and 36 Experimental Results: diminished tumor growth. |
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| References |
| Molecular Formula |
C19H12CL3N3OS
|
|---|---|
| Molecular Weight |
436.7421
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| Exact Mass |
434.977
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| Elemental Analysis |
C, 52.25; H, 2.77; Cl, 24.35; N, 9.62; O, 3.66; S, 7.34
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| CAS # |
338404-52-7
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| PubChem CID |
3751173
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.48g/cm3
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| Index of Refraction |
1.697
|
| LogP |
6.573
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
520
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C1=C(/C(/[H])=N/OC([H])([H])C2C([H])=C([H])C(=C(C=2[H])Cl)Cl)N2C([H])=C([H])SC2=N1
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| Synonyms |
CITCO
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~57.24 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2897 mL | 11.4485 mL | 22.8969 mL | |
| 5 mM | 0.4579 mL | 2.2897 mL | 4.5794 mL | |
| 10 mM | 0.2290 mL | 1.1448 mL | 2.2897 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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