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.
|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 models||Human breast (MDA-MB-231) tumor-bearing mice|
|Dosages||5 mg/kg every 2 or every 3 days|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Source||Liver Int (2012). Figure 1. NSC 74859|
|Cell Lines||Non-small cell|
|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)|
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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