NSC 74859 (S31-201) is a STAT3 inhibitor and is effective in hepatocellular cancers with disrupted TGF-beta signaling.Both CD133 (+) Huh-7 cells and CD133 (-) Huh-7 cells are equally sensitive to NSC 74859 treatment and STAT3 inhibition, with an IC (50) of 100 muM.Furthermore, NSC 74859 (S31-201) treatment of Huh-7 xenografts in nude mice significantly retarded tumor growth, with an effective dose of only 5 mg/kg. Moreover, NSC 74859 (S31-201) inhibited tyrosine phosphorylation of STAT3 in HCC cells in vivo.*The compound is unstable in solutions, freshly prepared is recommended
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Source | Liver Int (2012). Figure 1. NSC 74859 |
| Method | MTT assay | |
| Cell Lines | Non-small cell | |
| Concentrations | 100 μM | |
| Incubation Time | 48 h | |
| Results | Cell viability of hepatoma cells treated with a combination of cetuximab and 100 μM of NSC 74859 decreased significantly, when compared with hepatoma cells treated with cetuximab alone (when the concentration of cetuximab >100 mg/ml, P < 0.0001 for all cell lines) |
| Cell Experiment | |
|---|---|
| Cell lines | NIH 3T3, NIH 3T3/v-Src, MDA-MB-453, MDA-MB-435, MDA-MB-231, or MDA-MB-468 cells line |
| Preparation method | Measurement of Apoptosis by Flow Cytometry. Proliferating cells were treated with or without S3I-201 for up to 48 h. In some cases, cells were first transfected with Stat3C, ST3-NT, or ST3-SH2 domain or mock-transfected for 24 h before treatment with compound for an additional 24-48 h. Cells were then detached and analyzed by annexin V binding (BD Biosciences, San Diego, CA) according to the manufacturer's protocol and flow cytometry to quantify the percent apoptosis. |
| Concentrations | 100 μ M |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Human breast (MDA-MB-231) tumor-bearing mice |
| Formulation | normal saline |
| Dosages | 5 mg/kg every 2 or every 3 days |
| Administration | i.v. |
| Molecular Weight | 365.36 |
| Formula | C16H15NO7S |
| CAS Number | 501919-59-1 |
| Solubility (25°C) | DMSO 73 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related STAT Products |
|---|
| STAT3-IN-21, cell-permeable, negative control
STAT3-IN-21, cell-permeable, negative control, a peptide, is a negative control for Stat3 activity detection. |
| STAT3-IN-24, cell-permeable
STAT3-IN-24, cell-permeable (PpYLKTK-mts) is a STAT3 peptide inhibitor. |
| 5-FAM-GpYLPQTV-NH2
5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide and has STAT3 inhibitory activity. |
| Ac-GpYLPQTV-NH2
Ac-GpYLPQTV-NH2 is a STAT3 inhibitor with an IC50 value of 0.33 μM. |
| XZH-5
XZH-5 inhibits the phosphorylation of STAT3 and results in the induction of apoptosis and reduction of colony forming ability. |
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