LQZ-7I

Product NameLQZ-7I
CAS195822-23-2
MFC20H14F2N4
MW348.35
EINECS
MOL File195822-23-2.mol

Chemical Properties

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

Usage And Synthesis

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

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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.

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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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