CZL-S092
CZL-S092 is a PLK4 inhibitor with an IC50 value of 0.9 nM and excellent selectivity over other PLK4 family members (PLK1, PLK2, and PLK3). CZL-S092 exhibits anti-neuroblastoma activity in vitro (IMR-32 cells, IC50 = 1.143 μM). CZL-S092 inhibits cell migration and halts the cell cycle and induces apoptosis. CZL-S092 can be used in studies of various cancers including neuroblastoma cancer.
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- Formule: C23H19FN4OS
- Masse moléculaire:418.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PLK4 0.9 nM (IC50) |
In Vitro
CZL-S092 (0.5 μM; 60 min) inhibits PLK4 by > 80 % in a panel of 37 kinases and exhibits excellent selectivity over other PLK family members (PLK1, PLK2, and PLK3)[1].
CZL-S092 (0.5-2.5 μM,5 d) exhibits the optimal antiproliferative activity against MCF-7, IMR-32 and SH-SY5Y cells with IC50 values of 2.828 μM, 1.143 μM, and 1.329 μM, respectively[1].
CZL-S092 (0.5-5 μM; 48 h) induces significant apoptosis (84.3%) in IMR-32 neuroblastoma cells[1].
CZL-S092 (2.5 μM; 48 h) arrestes IMR-32 cells at G2/M phase (87.4%)[1].
CZL-S092 (5.0 μM; 24 h) significantly suppresses IMR-32 cell migration ( > 90%) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, IMR-32, SH-SY5Y
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Concentration:0.5 μM, 1.0 μM, 2.5 μM
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Incubation Time:5 days
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Result:Exhibited the optimal antiproliferative activity against MCF-7, IMR-32 and SH-SY5Y cells with IC50 values of 2.828 μM, 1.143 μM, and 1.329 μM, respectively.
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Cell Line:IMR-32
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Concentration:1.0 μM, 2.5 μM, 5.0 μM
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Incubation Time:48 h
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Result:Produced a remarkable 87.4% and 89.6% G2/M phase arrest at a concentration of 2.5 μM and 5.0 μM.
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Cell Line:IMR-32
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Concentration:1.0 μM, 2.5 μM, 5.0 μM
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Incubation Time:48 h
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Result:Induced the total rate to 84.3% at a concentration of 2.50 μM, and 90.2% at 5.0 μM.
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Cell Line:IMR-32
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Concentration:1.0 μM, 2.5 μM, 5.0 μM
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Incubation Time:24 h
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Result:Significantly suppressed over 90% of the wound healing with 5.0 μM.
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Cell Line:IMR-32
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Concentration:2.5 μM
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Incubation Time:48 h
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Result:Occurred disordered centrosome replication and resulted in centriole loss. T.
Parmacokinetics
| Species | Dose | Route | AUC0-t | CL | Vss | T1/2 | MRT0-t | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat | 1 mg/kg | i.v. | 466 ng·h/mL | 35.6 mL/min/kg | 0.955 L/kg | 0.769 h | 0.414 h | / | / | / |
| Rat | 10 mg/kg | i.g. | 1030 ng·h/mL | / | / | 0.387 h | 0.935 h | 917 ng/mL | 0.5 h | 22.1 % |
Chemical Information
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Masse moléculaire 418.49
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Formule C23H19FN4OS
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SMILES
CN(C1=CC=CC(F)=C1)C(CSC2=CC3=C(C(/C=C/C4=CC=CN=C4)=NN3)C=C2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CZL-S092 Related Classifications
HY-176734 Related Classifications
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