LQZ-7I

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[1].

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> Survivin

Survivin[1]

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[1]. 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[1]. Western Blot Analysis[1] 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[1]. Animal Model: 6-week old male NSG mice[1] 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.

[1]. Robert Peery,et al. Synthesis and Identification of a Novel Lead Targeting Survivin Dimerization for Proteasome-Dependent Degradation. J Med Chem. 2020 Jun 9.