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195822-23-2

195822-23-2 Structure

195822-23-2 Structure
IdentificationBack 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 PropertiesBack 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
Safety DataBack Directory
[Symbol(GHS) ]


GHS05,GHS07
[Signal word ]

Danger
[Hazard statements ]

H302+H312+H332-H314
[Precautionary statements ]

P501-P261-P270-P271-P264-P280-P362+P364-P303+P361+P353-P301+P330+P331-P301+P312+P330-P304+P340+P310-P305+P351+P338+P310-P405
Hazard InformationBack 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

< tr>
Cell Line: PC- 3 or C4-2 cells
Concentration: 10 μM
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.

td>
Animal Model: 6-week old male NSG mice
Dosage: 100 mg/kg; 200 μL vehicle (90% corn oil/10% DMSO)
Administration: 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]

Survivin

[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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