195822-23-2
中文名稱
N2,N3-雙(4-氟苯基)喹喔啉-2,3-二胺
英文名稱
LQZ-7I
CAS
195822-23-2
分子式
C20H14F2N4
分子量
348.35
MOL 文件
195822-23-2.mol
更新日期
2025/01/07 01:12:43
195822-23-2 結(jié)構(gòu)式
基本信息
中文別名
化合物L(fēng)QZ-7IN2,N3-雙(4-氟苯基)喹喔啉-2,3-二胺
英文別名
LQZ-7IN2,N3-Bis(4-fluorophenyl)quinoxaline-2,3-diamine
2,3-Quinoxalinediamine, N2,N3-bis(4-fluorophenyl)-
所屬類別
醫(yī)藥中間體：喹啉類化合物物理化學(xué)性質(zhì)
熔點203 °C(Solv: ethanol (64-17-5))
沸點470.3±45.0 °C(Predicted)
密度1.390±0.06 g/cm3(Predicted)
儲存條件Keep in dark place,Inert atmosphere,Room temperature
溶解度DMSO: 125 mg/mL (358.83 mM)
酸度系數(shù)(pKa)2.56±0.59(Predicted)
形態(tài)A solid
顏色Light yellow to green yellow
常見問題列表
生物活性
LQZ-7I 是一種靶向 survivin 的抑制劑。LQZ-7I 抑制生存素二聚化。LQZ-7I 口服有效抑制異種移植腫瘤生長并誘導(dǎo)腫瘤中生存素的損失。靶點
Survivin
體外研究
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. |
體內(nèi)研究
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. |