生物活性 靶点 体外研究 体内研究
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CITCO

生物活性 靶点 体外研究 体内研究
CITCO,338404-52-7,结构式
CITCO
  • CAS号:338404-52-7
  • 英文名:CITCO
  • 中文名:CITCO
  • CBNumber:CB4497318
  • 分子式:C19H12Cl3N3OS
  • 分子量:436.74
  • MOL File:338404-52-7.mol
CITCO化学性质
  • 密度 :1.48±0.1 g/cm3(Predicted)
  • 储存条件 :-20°C
  • 溶解度 :DMSO: 28 mg/mL, soluble
  • 形态 :solid
  • 酸度系数(pKa) :4.05±0.40(Predicted)
安全信息
  • 危险品标志 :Xi
  • 危险类别码 :36/37/38
  • 安全说明 :26-36
  • WGK Germany :3

CITCO性质、用途与生产工艺

  • 生物活性 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。
  • 靶点

    CAR, PXR

  • 体外研究

    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

    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

    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

    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

    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

    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 .

    Animal Model: Six- to eight-week-old male athymic nude mice
    Dosage: 25 or 100 μg
    Administration: Intraperitoneal; on days 22, 24, 26, 30 and 36
    Result: Decreased tumour growth.
CITCO上下游产品信息
上游原料
下游产品
CITCO生产厂家
  • 公司名称：上海喀露蓝科技有限公司
  • 联系电话： 18149758185
  • 电子邮件：sales-cpd@caerulumpharma.com
  • 国家：中国
  • 产品数：3421
  • 优势度：58
  • 公司名称：EMMX Biotechnology LLC
  • 联系电话：888-539-0666
  • 电子邮件：info@emmx.com
  • 国家：美国
  • 产品数：8449
  • 优势度：60
  • 公司名称：上海超岚化工科技中心
  • 联系电话：QQ:65489617 15618227136
  • 电子邮件：info@SuperLan-chem.com
  • 国家：中国
  • 产品数：9748
  • 优势度：58
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