1. Apoptosis
  2. Survivin Apoptosis
  3. LQZ-7F

LQZ-7F, a survivin dimerization inhibitor, induces spontaneous apoptosis and synergizes with Docetaxel in prostate cancer cells. LQZ-7F dose-dependently inhibits survival of both PC-3 and C4-2 cells with IC50s of 2.99 and 2.47 µM, respectively.

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LQZ-7F Chemical Structure

LQZ-7F Chemical Structure

CAS No. : 354543-09-2

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Based on 1 publication(s) in Google Scholar

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Description

LQZ-7F, a survivin dimerization inhibitor, induces spontaneous apoptosis and synergizes with Docetaxel in prostate cancer cells. LQZ-7F dose-dependently inhibits survival of both PC-3 and C4-2 cells with IC50s of 2.99 and 2.47 µM, respectively[1].

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.99 μM
Compound: 18, ZINC02092166
Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTS assay
Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTS assay
[PMID: 25985283]
HEK293 IC50
0.86 μM
Compound: 18, ZINC02092166
Inhibition of interaction of beta-catenin (unknown origin) transfected in Wnt-activated HEK293 cells/Tcf4 assessed as decrease in transactivation of canonical Wnt signaling by TOPflash luciferase reporter assay
Inhibition of interaction of beta-catenin (unknown origin) transfected in Wnt-activated HEK293 cells/Tcf4 assessed as decrease in transactivation of canonical Wnt signaling by TOPflash luciferase reporter assay
[PMID: 25985283]
HT-29 IC50
1.1 μM
Compound: 18, ZINC02092166
Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTS assay
Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTS assay
[PMID: 25985283]
SW480 IC50
0.71 μM
Compound: 18, ZINC02092166
Inhibition of beta-catenin/Tcf4 interaction in human SW480 cells assessed as decrease in transactivation of canonical Wnt signaling by TOPflash luciferase reporter assay
Inhibition of beta-catenin/Tcf4 interaction in human SW480 cells assessed as decrease in transactivation of canonical Wnt signaling by TOPflash luciferase reporter assay
[PMID: 25985283]
SW480 IC50
0.85 μM
Compound: 18, ZINC02092166
Cytotoxicity against human SW480 cells assessed as inhibition of cell growth after 72 hrs by MTS assay
Cytotoxicity against human SW480 cells assessed as inhibition of cell growth after 72 hrs by MTS assay
[PMID: 25985283]
In Vitro

LQZ-7F could be hudrolyzed under acidic conditions[1].
LQZ-7F (2.5 μM, 72 hours) displays cytotoxicity towards human cancer cells (PC-3, C4-2) with the IC50s of 2.99 μM and 2.74 μM, respectively[1].
LQZ-7F effectively inhibits survival of all cancer cell lines with IC50 values ranging between 0.4 and 4.4 mM[2].
LQZ-7F (2 μM, 24 hours) disrupts microtubule structure and cause mitotic arrest in P3 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: PC3, HL-60 cells
Concentration: 0, 5, 10 μM
Incubation Time:
Result: Caused 54% to 69% apoptosis for PC3 and 66% to 98% apoptosis for HL-60 cells.

Cell Cytotoxicity Assay[1]

Cell Line: PC-3, DU145
Concentration: 10, 20 μM
Incubation Time: 72 hours
Result: Showed that the IC50 in human PC3 and DU145 cells was approximately 25 μM.
In Vivo

LQZ-7F (i.p. injection; 25 mg/kg once every 3 days; 24 days) inhibits growth of xenograft tumor and may be due to its induction of surviving degradation in vivo[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4- to 6-week-old male NSG (NOD/SCID/IL-2Rg null) mice[2].
Dosage: 25 mg/kg
Administration: 24 days
Result: Inhibited growth of xenograft tumors by inhibiting surviving.
Molecular Weight

349.26

Formula

C14H7N9O3

CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(C1=NON=C1N)N/N=C2C3=C(C4=NC5=NON=C5N=C4\2)C=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (14.32 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8632 mL 14.3160 mL 28.6320 mL
5 mM 0.5726 mL 2.8632 mL 5.7264 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8632 mL 14.3160 mL 28.6320 mL 71.5799 mL
5 mM 0.5726 mL 2.8632 mL 5.7264 mL 14.3160 mL
10 mM 0.2863 mL 1.4316 mL 2.8632 mL 7.1580 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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LQZ-7F
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HY-122678
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