LQZ-7I is a malarial protease PfSUB1 inhibitor. LQZ-7I showed significantly improved activity and is the focus of this work. LQZ-7 when given orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors. The data obtained utilizing LQZ-7I in both in vitro and in vivo studies highlights its potential as a lead for further development, which may yield a potential cancer therapeutic by targeting the survivin protein directly.
CAS Number: 195822-23-2
Molecular Weight: 348.35
Chemical Name: 2,3-Quinoxalinediamine, N,N'-bis(4-fluorophenyl)-
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
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.
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.
- Peery, Robert; Kyei-Baffour, Kwaku; Dong, Zizheng; Liu, Jianguo; de Andrade Horn, Pedro; Dai, Mingji; Liu, Jing-Yuan; Zhang, Jian-Ting Synthesis and Identification of a Novel Lead Targeting Survivin Dimerization for Proteasome-Dependent Degradation, Journal of Medicinal Chemistry (2020), Ahead of Print.
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