KB-15
KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer.
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- Fòrmula: C18H12Cl4N2O2
- Peso molecular:430.11
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Almacenamiento:
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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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
KB-15 (72 h) exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM)[1].
KB-15 (0.25-2 μM, 14 days) shows potent colony formation inhibitory activity against AGS and BGC-823 gastric cancer cells[1].
KB-15 (0.5-2 μM, 24 h) demonstrates potent ROS-inducing activity in BGC-823 cells[1].
KB-15 (0.25-2 μM, 24-36 h) exhibits potent G0/G1 phase arrest activity and induces apoptosis in AGS and BGC-823 cells[1].
KB-15 (0.5-2 μM, 24 h) inhibits STAT3 activation in a concentration-dependent manner and downregulates HO-1 in BGC-823 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AGS and BGC-823 cells
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Concentration:0.25, 0.5, 1, 2 μM
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Incubation Time:36 h
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Result:Induced concentration-dependent increase in the proportion of G0/G1 phase cells.
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Cell Line:BGC-823 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:24 h
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Result:Increased the total apoptosis rate in a concentration-dependent manner.
Upregulated pro-apoptotic proteins Cleaved-PARP and Bax.
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Cell Line:BGC-823 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:24 h
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Result:Inhibited STAT3 activation in a concentration-dependent manner and downregulated HO-1.
| Species | Dose | Route | T1/2 | Cmax | Tmax | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | i.p. | 2.33 h | 659 ng/mL | 0.333 h | 1.167 ng/L.h | 1.175 ng/L.h | 1.60 h | 1.70 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BGC-823 cells (5 × 107 in serum-free medium) were subcutaneously implanted into the left axillary area of 6-week-old male BALB/c (nu/nu) nude mice[1]
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Dosage:2.5 mg/kg
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Administration:i.p. once daily for 14 consecutive days
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Result:Achieved a tumor growth inhibition (TGI) rate of 53.3% at a dose of 2.5 mg/kg.
Reduced the expression of phosphorylated STAT3 (p-STAT3) and HO-1 protein in BGC-823 xenograft tumor tissues.
Increased the expression of pro-apoptotic proteins Cleaved-PARP and Bax, and decreased the expression of apoptotic protease Procaspase-3 in tumor tissues.
Chemical Information
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Peso molecular 430.11
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Fòrmula C18H12Cl4N2O2
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SMILES
ClC1=C(Cl)C=CC(/C=C/C(NNC(/C=C/C2=CC(Cl)=C(Cl)C=C2)=O)=O)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KB-15 Related Classifications
HY-175542 Related Classifications
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