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Submit ReviewInhibitor of gp130 (IC50 = 0.72 μM); blocks cytokine-triggered gp130 signaling. Induces gp130 phosphorylation and down regulates gp130 glycosylation; also abrogates STAT3 phosphorylation, nuclear translocation and inhibits the expression of downstream target genes. Delays tumor growth in a mouse xenograft model of human ovarian cancer. Orally active.
SC 144 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
M. Wt | 358.76 |
Formula | C16H11FN6O.HCl |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 917497-70-2 |
PubChem ID | 66921431 |
InChI Key | LKFGGXYXFIICED-UHFFFAOYSA-N |
Smiles | O=C(C4=CN=CC=N4)NNC1=NC(C=C(F)C=C3)=C3N2C1=CC=C2.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 32.23 | 100 |
The following data is based on the product molecular weight 358.76. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.79 mL | 13.94 mL | 27.87 mL |
5 mM | 0.56 mL | 2.79 mL | 5.57 mL |
10 mM | 0.28 mL | 1.39 mL | 2.79 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
References are publications that support the biological activity of the product.
Xu et al (2013) Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol.Cancer Ther. 12 937 PMID: 23536726
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.