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LQZ-7I is a surviving-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors[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

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]

[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.

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