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CITCO

目录号 : GC17491

An agonist of human CAR

CITCO Chemical Structure

Cas No.:338404-52-7

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5mg
¥649.00
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10mg
¥1,020.00
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25mg
¥1,854.00
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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].

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].

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].

References:
[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.

化学性质

Cas No. 338404-52-7 SDF
化学名 (E)-6-(4-chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime
Canonical SMILES ClC1=CC=C(C=C1)C2=C(/C=N/OCC(C=C3Cl)=CC=C3Cl)N4C(SC=C4)=N2
分子式 C19H12Cl3N3OS 分子量 436.74
溶解度 DMF: 20 mg/ml,DMSO: 10 mg/ml 储存条件 Desiccate at -20°C
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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 0.229 mL 1.1448 mL 2.2897 mL
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