N2,N3-双(4-氟苯基)喹喔啉-2,3-二胺
| 中文名称 | N2,N3-双(4-氟苯基)喹喔啉-2,3-二胺 |
|---|---|
| 中文同义词 | N2,N3-双(4-氟苯基)喹喔啉-2,3-二胺;化合物LQZ-7I |
| 英文名称 | LQZ-7I |
| 英文同义词 | LQZ-7I;2,3-Quinoxalinediamine, N2,N3-bis(4-fluorophenyl)-;N2,N3-Bis(4-fluorophenyl)quinoxaline-2,3-diamine;LQZ7I,inhibit,Survivin,LQZ 7I,Inhibitor,tumor,LQZ-7I,dimerization |
| CAS号 | 195822-23-2 |
| 分子式 | C20H14F2N4 |
| 分子量 | 348.35 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 195822-23-2.mol |
| 结构式 |  |
N2,N3-双(4-氟苯基)喹喔啉-2,3-二胺 性质
| 熔点 | 203 °C(Solv: ethanol (64-17-5)) |
|---|---|
| 沸点 | 470.3±45.0 °C(Predicted) |
| 密度 | 1.390±0.06 g/cm3(Predicted) |
| 储存条件 | Keep in dark place,Inert atmosphere,Room temperature |
| 溶解度 | 二甲基亚砜：125 mg/mL（358.83 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 2.56±0.59(Predicted) |
| 颜色 | 浅黄至黄绿色 |
LQZ-7I 是一种靶向 survivin 的抑制剂。LQZ-7I 抑制生存素二聚化。LQZ-7I 口服有效抑制异种移植肿瘤生长并诱导肿瘤中生存素的损失。
Survivin
LQZ-7I has improved cytotoxicity with IC
50
s of 3.1 µM against C4-2 cells and 4.8 µM against PC-3 cells compared with the parent compound LQZ-7.
LQZ-7I (10 µM; 0-6 hours) treatment reduces the expression of survivin. However, LQZ-7I does not reduce the expression of XIAP, CIAP1, and CIAP2. LQZ-7I may be selective to its intended target survivin.
Western Blot Analysis
| Cell Line: | PC-3 or C4-2 cells |
| Concentration: | 10 µM |
| Incubation Time: | 0-6 hours |
| Result: | Reduced the expression of survivin. |
LQZ-7I (100 mg/kg; oral gavage every other day for a total of ten treatments) significantly suppresses tumor growth without any notable adverse effect on the mice.
| Animal Model: | 6-week old male NSG mice |
| Dosage: | 100 mg/kg; 200 µL vehicle (90% corn oil/10% DMSO) |
| Administration: | Oral gavage every other day for a total of ten treatments |
| Result: | Significantly suppressed tumor growth without any notable adverse effect on the mice as indicated by lacking changes in body weight and in wet weight of major organs at the end of the study. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-136538 | LQZ-7I | 1 mg | 380元 | |
| 2024/11/08 | HY-136538 | N2,N3-双(4-氟苯基)喹喔啉-2,3-二胺 LQZ-7I | 195822-23-2 | 5mg | 600元 |