CITCO

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CITCO  纯度: 99.17%

CITCO 是一种组成型雄甾烷 (Constitutive androstane) 受体激动剂，抑制脑肿瘤干细胞 (BTSCs) 的生长和扩增。CITCO 是一种咪唑并噻唑衍生物，其作为人 CAR 的选择性激动剂起作用。CITCO 对于孕烷 X 受体 (PXR) 的 EC50 为 49 nM，并且对其他核受体没有活性。

CITCO

CITCO Chemical Structure

CAS No. : 338404-52-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1845 In-stock
5 mg ￥1675 In-stock
10 mg ￥2680 In-stock
25 mg ￥5360 In-stock
50 mg ￥8580 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CITCO 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Targeted Diversity Library

生物活性

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]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

436.74

Formula

C19H12Cl3N3OS
CAS 号

338404-52-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (57.24 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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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