Biological Activity
Potent kinesin spindle protein (KSP) inhibitor (Ki = 0.1 nM). Induces cell mitotic arrest and apoptosis in vitro. Inhibits the growth of a range of tumor cells in vitro, including colon (HCT 116), prostate (PC-3) and leukemia (K-562) cancer cell lines. Causes tumor regression in human tumor xenograft models in vivo, including colon (Colo205), lung (H69) and breast (MCF7) cancer cell xenografts.
Licensing Information
Sold with the permission of GlaxoSmithKline.
Compound Libraries
SB 743921 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 553.52 |
| Formula | C31H33ClN2O3.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 940929-33-9 |
| PubChem ID | 49867937 |
| InChI Key | MLMZVWABFOLFGV-LNLSOMNWSA-N |
| Smiles | ClC1=CC=C2C(OC([C@@H]([C@H](C)C)N(C(C4=CC=C(C)C=C4)=O)CCCN)=C(CC3=CC=CC=C3)C2=O)=C1.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 | 55.35 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 553.52. 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 | 1.81 mL | 9.03 mL | 18.07 mL |
| 5 mM | 0.36 mL | 1.81 mL | 3.61 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.81 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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References
References are publications that support the products' biological activity.
Jackson et al (2006) A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. First AACR International Conference on Molecular and Diagnostics in Cancer Therapeutic Development. Abstract (B11) PMID:
Good et al (2013) Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. J.Med.Chem. 56 1878 PMID: 23394180
Talapatra et al (2013) Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism. J.Med.Chem. 56 6317 PMID: 23875972
Keywords: SB 743921 hydrochloride, supplier, SB743921, hydrochloride, potent, kinesin, spindle, protein, inhibitors, inhibits, KSP, EG5, antitumor, apoptosis, Kinesin, Kinesin, Tocris Bioscience
