Biological Activity
Inhibitor 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.
Compound Libraries
SC 144 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 358.76 |
| Formula | C16H11FN6O.HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.23 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 358.76. Batch specific molecular weights may vary from batch to batch due to solvent 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
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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