666859-49-0
|
|
- CAS号:
- 666859-49-0
- 英文名:
- Methanone, (4-fluorophenyl)[1-[2-methoxy-2-(4-nitrophenyl)ethyl]-4-piperidinyl]-
- 英文别名:
- Telomerase-IN-1;Telomerase IN 1,TelomeraseIN1;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)
- 中文名:
- 666859-49-0
- 中文别名:
- 端粒酶-IN-1;化合物 T12009
- CBNumber:
- CB63339677
- 分子式:
- C21H23FN2O4
- 分子量:
- 386.4167232
- MOL File:
- 666859-49-0.mol
|
|
|
666859-49-0化学性质
-
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)
-
|
-
形态:
-
Solid
-
|
-
颜色:
-
Off-white to light yellow
-
|
666859-49-0性质、用途与生产工艺
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.
666859-49-0
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/08/19 | HY-U00268 | Telomerase-IN-1 | | 1 mg | 1136元 |
2024/08/19 | HY-U00268 | Telomerase-IN-1 | | 5 mg | 2500元 |
666859-49-0, 666859-49-0 相关搜索:
- 化合物 T12009
- 端粒酶-IN-1
- 666859-49-0
- Telomerase IN 1,TelomeraseIN1
- Telomerase-IN-1
- (4-fluorophenyl)(1-(2-methoxy-2-(4-nitrophenyl)ethyl)piperidin-4-yl)methanone(WXG03041)
- Methanone, (4-fluorophenyl)[1-[2-methoxy-2-(4-nitrophenyl)ethyl]-4-piperidinyl]-