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。
货号:ajcx29470
CAS:195822-23-2
分子式:C20H14F2N4
分子量：348.35
溶解度:DMSO: 125 mg/mL (358.83 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.