CITCO
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- CAS号:
- 338404-52-7
- 英文名:
- CITCO
- 英文别名:
- CITCO,Inhibitor,inhibit,Apoptosis;6-(4-Chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime;Imidazo[2,1-b]thiazole-5-carboxaldehyde, 6-(4-chlorophenyl)-, O-[(3,4-dichlorophenyl)methyl]oxime
- 中文名:
- CITCO
- 中文别名:
- 化合物CITCO;6-(4-氯苯基)咪唑并[2,1-B]噻唑-5-甲醛 O-(3,4-二氯苄基)肟
- CBNumber:
- CB4497318
- 分子式:
- C19H12Cl3N3OS
- 分子量:
- 436.74
- MOL File:
- 338404-52-7.mol
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CITCO化学性质
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密度:
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1.48±0.1 g/cm3(Predicted)
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储存条件:
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-20°C
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溶解度:
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DMSO: 28 mg/mL, soluble
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形态:
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solid
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酸度系数(pKa):
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4.05±0.40(Predicted)
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颜色:
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Light yellow to yellow
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CITCO性质、用途与生产工艺
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 (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.
CITCO (2.5, 5 μM; 48 hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes.
CITCO (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in culture in dose dependently, but not in normal astrocytes.
CITCO (0-25 μM; 48 hours) causes the T98G and U87MG glioma and BTSCs expressing very low levels of CAR protein that increased significantly.
Cell Proliferation Assay
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Cell Line:
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T98G, U87MG, DB29 and DB33 human glioma cells, astrocytes
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Concentration:
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1, 2.5, 5, 10, 25, 50 μM
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Incubation Time:
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48 hours
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Result:
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Resulted in a dose-dependent inhibition of viable cell count and proliferation.
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Cell Cycle Analysis
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Cell Line:
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The T98G, U87MG, DB29 and DB33 glioma cells
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Concentration:
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2.5, 5 μM
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Incubation Time:
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48 hours
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Result:
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Induced cell cycle arrest differentially in different BTSCs in culture.
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Apoptosis Analysis
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Cell Line:
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The T98G, U87MG, DB29 and DB33 glioma cells
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Concentration:
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2.5, 5 or 10 μM
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Incubation Time:
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48 hours
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Result:
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Increased the levels of Annexin V-positive apoptotic cells in dose dependently.
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Western Blot Analysis
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Cell Line:
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T98G, U87MG, DB29 and DB33 glioma cells
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Concentration:
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0 to 25 μM
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Incubation Time:
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48 hours
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Result:
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The T98G, U87MG glioma and BTSCs expressed very low levels of CAR protein that increased significantly.
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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 .
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Animal Model:
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Six- to eight-week-old male athymic nude mice
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Dosage:
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25 or 100 μg
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Administration:
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Intraperitoneal; on days 22, 24, 26, 30 and 36
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Result:
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Decreased tumour growth.
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CITCO
上下游产品信息
上游原料
下游产品
338404-52-7, CITCO 相关搜索:
- 合成有机化合物配体
- C19H12N3OCl3S
- 化合物CITCO
- 6-(4-氯苯基)咪唑并[2,1-B]噻唑-5-甲醛 O-(3,4-二氯苄基)肟
- 338404-52-7
- CITCO,Inhibitor,inhibit,Apoptosis
- 6-(4-Chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime
- Imidazo[2,1-b]thiazole-5-carboxaldehyde, 6-(4-chlorophenyl)-, O-[(3,4-dichlorophenyl)methyl]oxime