STAT3-IN-52
STAT3-IN-52 is an orally active STAT3 inhibitor with a Ki value of 2.42 μM. STAT3-IN-52 binds directly and selectively to the pY705 site of STAT3 (Ki = 0.44 μM), thereby impairing its function. STAT3-IN-52 induces apoptosis and triggers anti-tumor responses in vivo. STAT3-IN-52 can be used in breast cancer-related research.
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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
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Biologische Aktivität
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STAT3 2.42 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| 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] |
STAT3-IN-52 (Compound 9) selectively binds to the pY705 site of purified STAT3 protein with a Ki of 0.44 μM, and exhibits no binding activity toward purified STAT1 or STAT5 proteins[1].
STAT3-IN-52 binds directly to fluorescently labeled purified STAT3 protein, with a Ki value of 2.42 μM at a ligand-to-protein molar ratio of 1:1[1].
STAT3-IN-52 (0-400 μM; 24 h) inhibits the viability of human normal mammary epithelial MCF-10A cells, with an IC50 of 128.9 μM, and its potency against normal cells is 184-fold lower than that against MDA-MB-231 cancer cells[1].
STAT3-IN-52 (0.1-10 μM; 24 h) inhibits the viability of human basal-like breast cancer MDA-MB-231 cells, with an IC50 value of 0.7 μM[1].
STAT3-IN-52 (0.1-10 μM; 24 h) inhibits the viability of human medulloblastoma (UW426, UW288-1), human pancreatic cancer (BKPC3), human osteosarcoma (U2OS), and mouse sarcoma (S180) cells, with an IC50 of 0.42 μM against S180 cells[1].
STAT3-IN-52 (5 μM; 0-24 h) time-dependently and selectively inhibits the DNA-binding activity of STAT3 homodimers in human basal-like breast cancer MDA-MB-231 cells, exerts weak effects on STAT1 dimer binding, and does not inhibit IFN-γ-induced STAT1 binding or STAT5 dimer binding[1].
STAT3-IN-52 reduces the mRNA expression of the oncogene MMP9 in human basal-like breast cancer MDA-MB-231 cells, but exerts no significant effect on the expression of the CDK2 gene in these cells[1].
STAT3-IN-52 (2.5-10 μM; 12 h) dose-dependently reduces the level of p-STAT3Y705, inhibits IL-6-induced STAT3 phosphorylation, upregulates SHP-1 expression and induces the production of cleaved caspase-3 in human basal-like breast cancer MDA-MB-231 cells, without affecting other modification sites of STAT3, total STAT3, or the phosphorylation of AKT, ERK1/2 or STAT1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human basal-like breast cancer MDA-MB-231 cells
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Concentration:2.5, 5 and 10 μM
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Incubation Time:12 h; 2 h pre-incubation before 30 min IL-6 stimulation
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Result:Reduced the level of p-STAT3 (Y705) in a dose-dependent manner, without altering levels of acetylated STAT3 (K685), p-STAT3 (S727), total STAT3, p-AKT, or p-ERK1/2.
Inhibited IL-6-induced phosphorylation of STAT3, but did not inhibit p-STAT1 (Y701) or IFN-γ-induced phosphorylation of STAT1.
Increased the expression of SHP-1 and cleaved caspase-3.
| 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 | 198 ng·h/mL | 199.2 ng·h/mL | 4944.2 mL/kg | 5261.7 mL/h/kg | 0.55 h | 0.71 h | 44.7 % |
| Rat[1] | 10 mg/kg | p.o. | 1.98 h | 0.5 h | 540.3 ng/mL | 850 ng·h/mL | 889 ng·h/mL | 32092.5 mL/kg | 11766.8 mL/h/kg | 1.87 h | 2.25 h | / |
STAT3-IN-52 (5 mg/kg; p.o.; daily; 21 days) orally reduces S180 sarcoma xenograft weight by 73% with minimal systemic toxicity[1].
STAT3-IN-52 (200-1000 mg/kg; i.p.; single dose) exhibits very low acute toxicity in ICR mice, with an estimated therapeutic index of over 100[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (6-week-old female, athymic SPF, subcutaneous xenograft of human MDA-MB-231 breast cancer cells)[1]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 32 days
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Result:Reduced tumor weight by 53% at 2.5 mg/kg, 60% at 5 mg/kg, and 70% at 10 mg/kg.
Showed normal body weight gain, with no damage to major organs (heart, liver, spleen, lung, kidney) detected via H&E staining.
Dose-dependently inhibited p-STAT3 (Y705) levels in tumor tissue, with no significant effect on total STAT3 levels, as confirmed by immunohistochemical analysis and Western blot.
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Animal Model:ICR (4-week-old male, subcutaneous xenograft of mouse S180 sarcoma cells)[1]
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Dosage:5 mg/kg
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Administration:p.o.; daily; 21 days
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Result:Reduced tumor weight by 73% after 21 days of treatment.
Showed normal body weight gain, in contrast to dramatic weight loss observed in doxorubicin-treated mice starting on day 13.
Organs (liver, spleen, kidney) were notably larger than those from doxorubicin-treated mice, indicating less toxicity.
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)
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