666859-49-0

666859-49-0

中文名称666859-49-0
中文同义词端粒酶-IN-1;化合物 T12009
英文名称Methanone, (4-fluorophenyl)[1-[2-methoxy-2-(4-nitrophenyl)ethyl]-4-piperidinyl]-
英文同义词Methanone, (4-fluorophenyl)[1-[2-methoxy-2-(4-nitrophenyl)ethyl]-4-piperidinyl]-;(4-fluorophenyl)(1-(2-methoxy-2-(4-nitrophenyl)ethyl)piperidin-4-yl)methanone(WXG03041);Telomerase-IN-1;Telomerase IN 1,TelomeraseIN1
CAS号666859-49-0
分子式C21H23FN2O4
分子量386.4167232
EINECS号
相关类别
Mol文件666859-49-0.mol
结构式666859-49-0 结构式

666859-49-0 性质

沸点512.7±50.0 °C(Predicted)
密度1.236±0.06 g/cm3(Predicted)
酸度系数(pKa)7.16±0.10(Predicted)

666859-49-0 用途与合成方法

Telomerase-IN-1 是一个端粒酶抑制剂,IC50 值为 0.19 μM。

IC50: 0.19 μM (Telomerase)

Our in vitro studies show that title compound (Telomerase-IN-1) has high inhibitory activity against telomerase and high antiproliferative capacity on SMMC-7721 cells, and has no obvious toxic effect on human normal hepatocyte cells. Telomerase-IN-1 treatment decreases the growth of cancer cells in dose- and time-dependent manners; however, the viability of L-02 shows slight changes in the compound at 10 μM. 48 h of SMMC-7721 cell treatment with the Telomerase-IN-1 (20, 40, and 80 nM) causes increase of apoptosis. Forty-eight hours of SMMC-7721 cell treatment with the Telomerase-IN-1(20, 40, and 80 nM) causes significant accumulation of green fluorescence, indicating a decrease in MMP. At 40 nM, Telomerase-IN-1 significantly increases expressions of cyt-c and Bax, but the Bcl-2 level is decreased.

Our in vivo studies show that this compound (Telomerase-IN-1) significantly inhibits tumor growth in xenograft tumor models. Results show that endoplasmic reticulum stress (ERS) through ER over response (EOR) activates the expression of hTERT, and then induces ERS, which is believed to be intricately associated with oxidative stress and mitochondrial dysfunction, resulting in apoptotic cell death, thereby modulating the expression of downstream signaling molecules including CHOP (CAAT/enhancer-binding protein homologous protein)) and mitochondrion pathway of apoptosis, leading to inhibition of cell proliferation.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-U00268Telomerase-IN-11 mg1136元
2024/01/25HY-U00268Telomerase-IN-15 mg2500元

666859-49-0 上下游产品信息

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