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.
Chemical Formula: C20H14F2N4
Exact Mass: 348.1187
Molecular Weight: 348.3568
Elemental Analysis: C, 68.96; H, 4.05; F, 10.91; N, 16.08
InChi Code: InChI=1S/C20H14F2N4/c21-13-5-9-15(10-6-13)23-19-20(24-16-11-7-14(22)8-12-16)26-18-4-2-1-3-17(18)25-19/h1-12H,(H,23,25)(H,24,26)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
Products are for research use only. Not for human use.
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