LQZ-7
LQZ-7 is a survivin inhibitor and molecular glue degrader (Kd=0.24 μM). LQZ-7 binds to the dimerization interface of survivin, disrupting homodimerization and dissociating dimeric survivin into monomers, thereby accelerating its proteasome-dependent degradation. LQZ-7 does not affect the structurally similar dimeric proteins 14-3-3σ and 14-3-3δ, and can induce apoptosis, exhibiting cytotoxicity against cancer cells.
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- CAS 番号: 1044664-73-4
- 分子式: C24H19N7O4
- 分子量:469.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
25 μM
|
Inhibitory concentration 50% against human PC-3 cancer cells assessed as reduction in cell survival incubated for 3 days by MTT assay.
Inhibitory concentration 50% against human PC-3 cancer cells assessed as reduction in cell survival incubated for 3 days by MTT assay.
|
26744521 |
| DU-145 | IC50 |
25 μM
|
Inhibitory concentration 50% against human DU145 cancer cells assessed as reduction in cell survival incubated for 3 days by MTT assay.
Inhibitory concentration 50% against human DU145 cancer cells assessed as reduction in cell survival incubated for 3 days by MTT assay.
|
26744521 |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DU145 and PC-3
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Concentration:25 µM
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Incubation Time:3 days
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Result:Inhibited survival of human PC-3 and DU145 cells with an IC50 of ~25 µM.
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Cell Line:PC-3
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Concentration:10 µM
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Incubation Time:24 hours
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Result:Induced survivin loss that was reversed by co-treatment with a proteasome inhibitor, MG132 or bortezomib.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (male, 4-6 weeks old)[1]
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Dosage:25 mg/kg
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Administration:i.p.; every 3 days; 8 doses
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Result:Inhibited the growth of PC-3 xenograft tumors compared to the vehicle control.
Reduced final average tumor weight significantly compared to the control group.
Maintained constant body weight after multiple dosings.
Induced apoptosis, showing more apoptotic cells with condensed chromatin.
Dramatically reduced survivin levels as determined by Western blot and immunohistochemistry.
化学情報
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CAS 番号 1044664-73-4
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分子量 469.45
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分子式 C24H19N7O4
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SMILES
OC(C1=CC=CC(C2=CC=C(O2)/C=N/NC3=NC4=NON=C4N=C3NC5=C(C(C)=CC=C5)C)=C1)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)