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NSC 74859

Cat. No. M1782
NSC 74859 Structure
Synonym:

S3I-201

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 80 In stock
50mg USD 250 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Customer Product Validations & Biological Datas
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)
Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 365.36
Formula C16H15NO7S
CAS Number 501919-59-1
Purity >98%
Solubility DMSO
Storage at -20°C
References

NSC 74859 enhances doxorubicin cytotoxicity via inhibition of epithelial-mesenchymal transition in hepatocellular carcinoma cells.
Hu QD, et al. Cancer Lett. 2012 Dec 28;325(2):207-13. PMID: 22781398.

NSC 74859-mediated inhibition of STAT3 enhances the anti-proliferative activity of cetuximab in hepatocellular carcinoma.
Chen W, et al. Liver Int. 2012 Jan;32(1):70-7. PMID: 22098470.

The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-beta signaling.
Lin L, et al. Oncogene. 2009 Feb 19;28(7):961-72. PMID: 19137011.

Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity.
Siddiquee K, et al. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7391-6. PMID: 17463090.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: NSC 74859, S3I-201 supplier, STAT, inhibitors

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