LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
IC50&Target
Survivin
体外研究
LQZ-7I has improved cytotoxicity with IC50s 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.
体内研究
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.
分子量
348.35
CAS号
195822-23-2
运输条件
Room temperature in continental US; may vary elsewhere.