STAT3-IN-46
STAT3-IN-46 is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3) (KD = 323.3 nM). STAT3-IN-46 directly binds to the SH2 domain of the STAT3 and inhibits IL-6/JAK/STAT3 signaling pathway (IC50 = 0.87 μM) and downregulates c-Myc and Bcl-2 levels. STAT3-IN-46 can be used for the research of cancer, such as triple-negative breast cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C31H29FN8S
- Peso molecular:564.68
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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
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
STAT3 323.3 nM (Kd) |
Bcl-2 |
IL-6 |
In Vitro
STAT3-IN-46 (Compound W36) shows anti-proliferative activity in MDA-MB-231 and MDA-MB-468 cells with IC50 values of 0.61 and 0.65 μM[1].
STAT3-IN-46 displays minimal cytotoxic effects in HEK293 and HK2 cells with IC50 values of 1.87 and 1.73 μM[1].
STAT3-IN-46 inhibits the IL-6/JAK/STAT3 signaling pathway in HEK-Blue-IL-6 cells with IC50 of 0.87 μM[1].
STAT3-IN-46 (2.5-10 μM, 6-12 h) inhibits levels of phosphorylated STAT3 in MDA-MB-231 and MDA-MB-468 cells[1].
STAT3-IN-46 (2.5-10 μM, 24 h) downregulates c-Myc and Bcl-2 levels in MDA-MB-231 and MDA-MB-468 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 and MDA-MB-468 cells
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Concentration:2.5, 5 and 10 μM
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Incubation Time:6, 12 and 24 h
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Result:Reduced p-STAT3 levels.
Did not affect STAT1 and STAT5 phosphorylation levels.
Downregulated c-Myc and Bcl-2 levels.
Parmacokinetics
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | T1/2 | Tmax | Cmax | Vz | CL | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2.5 mg/kg | i.v. | 1820.42 ng·h/mL | 2203.89 ng·h/mL | 3.85 h | 6.43 h | 4.61 h | 0.08 h | 530.47 ng/mL | 7.54 L/kg | 18.91 mL/min/kg | / |
| Rat[1] | 50 mg/kg | p.o. | 6798.54 ng·h/mL | 7448.32 ng·h/mL | 8.17 h | 10.35 h | 6.38 h | 4 h | 561.37 ng/mL | 61.81 L/kg | 111.98 mL/min/kg | 18.67 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-231 xenograft mice models[1]
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Dosage:7.5 and 10 mg/kg (Intraperitoneally injection) and 100 mg/kg (Orally administration)
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Administration:Daily for 16 days
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Result:Reduced tumor volume.
Had no body weight loss.
Chemical Information
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Peso molecular 564.68
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Fòrmula C31H29FN8S
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SMILES
N#CC1=CC=CC(C2=NN=C(NC3=C(N4CCN(CC)CC4)C=C5N(C6CC6)C(C7=CC=C(F)C=C7)=NC5=C3)S2)=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)
STAT3-IN-46 Related Classifications
HY-175771 Related Classifications
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