| Identification | Back Directory | [Name]
LQZ-7I | [CAS]
195822-23-2 | [Synonyms]
LQZ-7I
2,3-Quinoxalinediamine, N2,N3-bis(4-fluorophenyl)- | [Molecular Formula]
C20H14F2N4 | [MDL Number]
MFCD00607076 | [MOL File]
195822-23-2.mol | [Molecular Weight]
348.35 |
| Chemical Properties | Back Directory | [Melting point ]
203 °C(Solv: ethanol (64-17-5)) | [Boiling point ]
470.3±45.0 °C(Predicted) | [density ]
1.390±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,Room temperature | [solubility ]
DMSO: 125 mg/mL (358.83 mM) | [form ]
A solid | [pka]
2.56±0.59(Predicted) | [color ]
Light yellow to green yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
LQZ-7I is an inhibitor targeting survivin. It can inhibits survivin dimerization and xenograft tumor growth and induces loss of survivin in the tumor. | [in vitro]
LQZ-7I has improved cytotoxicity with IC 50 s 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 . Western Blot Analysis | Cell Line: | PC- 3 or C4-2 cells | | Concentration: | 10 μM | < tr> Incubation Time: | 0-6 hours | | Result: | Reduced the expression of survivin. | | [in vivo]
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. | Animal Model: | 6-week old male NSG mice | | Dosage: | 100 mg/kg; 200 μL vehicle (90% corn oil/10% DMSO) | | Administration: | td> 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. | | [target]
| [References]
[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. DOI:10.1021/acs.jmedchem.0c00475 |
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| Company Name: |
cjbscvictory
|
| Telephone: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
| Company Name: |
Bide Pharmatech Ltd.
|
| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
| Company Name: |
InvivoChem
|
| Telephone: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|