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.
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- 화학식: C31H29FN8S
- 분자량:564.68
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보관:
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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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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. Further protocols information, click here.
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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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분자량 564.68
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STAT3-IN-46 Related Classifications
HY-175771 Related Classifications
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