STAT3-IN-52
STAT3-IN-52 (Compound 9) is a selective and orally active signal transducer and activator of transcription 3 (STAT3) inhibitor. STAT3-IN-52 binds to the pY705 site of STAT3 (Ki = 440 nM), blocking the phosphorylation and dimerization of STAT3. STAT3-IN-52 shows strong cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 = 0.7 μM), medulloblastoma UW426, pancreatic cancer BKPC3 cells. STAT3-IN-52 can induce cell apoptosis, inhibit the STAT3 nuclear transport and DNA binding activity and downregulate the expression of the STAT3 target gene MMP9. STAT3-IN-52 can be used for research related to STAT3 abnormal activation in cancer.
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- CAS. Nr.: 1556861-34-7
- Formel: C20H20N4O4S
- Molecular Weight:412.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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STAT3 440 nM (Ki) |
MMP-9 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF S-180 | IC50 |
0.42 μM
Compound: 9
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Antiproliferative activity against human S180 cells after 24 hrs by MTT assay
Antiproliferative activity against human S180 cells after 24 hrs by MTT assay
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[PMID: 28245116] |
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | Vz | CL | MRT0-t | MRT0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 0.71 h | 0.033 h | 359.0 ng/mL | 189.0 ng·h/mL | 199.2 ng·h/mL | 4944.2 mL/kg | 5261.7 mL/h/kg | 0.55 h | 0.71 h | / |
| Rat[1] | 10 mg/kg | p.o. | 1.98 h | 0.5 h | 540.3 ng/mL | 850.0 ng·h/mL | 889.0 ng·h/mL | 32092.5 mL/kg | 11766.8 mL/h/kg | 1.87 h | 2.25 h | 44.7 % |
Chemical Information
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CAS. Nr. 1556861-34-7
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Molecular Weight 412.46
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Formel C20H20N4O4S
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SMILES
O=S(C(C=CC=C1C(C(NC2=CC=CC=C2N3CCNCC3)=C4)=O)=C1C4=O)(N)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
STAT3-IN-52 Related Classifications
HY-177990 Related Classifications
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