Biological Activity
High affinity allosteric kinesin spindle protein (KSP) inhibitor (Ki app = 1.7 nM). Exhibits >10,000-fold selectivity for KSP over a range of other mitotic kinesins. Inhibits proliferation and induces apoptosis of prostate and breast cancer cells in vitro. Induces tumor regression of breast cancer cell xenografts in mice.
Technical Data
| M. Wt | 517.06 |
| Formula | C30H33ClN4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 336113-53-2 |
| PubChem ID | 6851740 |
| InChI Key | QJZRFPJCWMNVAV-HHHXNRCGSA-N |
| Smiles | O=C2N(CC3=CC=CC=C3)C([C@@H]([C@@H](C)C)N(CCCN)C(C4=CC=C(C)C=C4)=O)=NC1=CC(Cl)=CC=C12 |
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 | 51.71 | 100 | |
| ethanol | 51.71 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 517.06. 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 | 1.93 mL | 9.67 mL | 19.34 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.87 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.93 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Lad et al (2008) Mechanism of inhibition of human KSP by ispinesib. Biochemistry 47 3576 PMID: 18290633
Davis et al (2006) Increased therapeutic potential of an experimental anti-mitotic inhibitor SB715992 by genistein in PC-3 human prostate cancer cell line. BMC Cancer 6 22 PMID: 16433906
Purcell et al (2010) Activity of the kinesin spindle protein inhibitor ispinesib (SB-715992) in models of breast cancer. Clin.Cancer Res. 16 566 PMID: 20068098
Keywords: Ispinesib, supplier, SB715992, CK0238273, high, affinity, selective, potent, allosteric, kinesin, spindle, protein, KSP, hsEG5, SB, 715992, Kinesin, Kinesin, Tocris Bioscience
