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338404-52-7

中文名稱 CITCO
英文名稱 CITCO
CAS 338404-52-7
分子式 C19H12Cl3N3OS
分子量 436.74
MOL 文件 338404-52-7.mol
更新日期 2024/04/26 14:13:12
338404-52-7 結(jié)構(gòu)式 338404-52-7 結(jié)構(gòu)式

基本信息

中文別名
化合物CITCO
6-(4-氯苯基)咪唑并[2,1-B]噻唑-5-甲醛 O-(3,4-二氯芐基)肟
英文別名
Imidazo[2,1-b]thiazole-5-carboxaldehyde, 6-(4-chlorophenyl)-, O-[(3,4-dichlorophenyl)methyl]oxime

物理化學(xué)性質(zhì)

密度1.48±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C
溶解度DMSO: 28 mg/mL, soluble
溶解度DMSO:28 mg/mL,可溶
酸度系數(shù)(pKa)4.05±0.40(Predicted)
形態(tài)solid
顏色Light yellow to yellow

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H315-H319-H335
危險(xiǎn)品標(biāo)志Xi
危險(xiǎn)類別碼36/37/38
安全說明26-36
WGK Germany3
WGK Germany3

圖譜信息

常見問題列表

生物活性
CITCO 是一種組成型雄甾烷 (Constitutive androstane) 受體激動(dòng)劑,抑制腦腫瘤干細(xì)胞 (BTSCs) 的生長(zhǎng)和擴(kuò)增。CITCO 是一種咪唑并噻唑衍生物,其作為人 CAR 的選擇性激動(dòng)劑起作用。CITCO 對(duì)于孕烷 X 受體 (PXR) 的 EC50 為 49 nM,并且對(duì)其他核受體沒有活性。
靶點(diǎn)

CAR, PXR

體外研究

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.
體內(nèi)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.
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