Catalog Number: 5109
Chemical Name: N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methylbenzamide hydrochloride
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.
Technical Data
  • M.Wt:
    553.52
  • Formula:
    C31H33ClN2O3.HCl
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    940929-33-9
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.
Additional Information
Licensing Caveats:
Sold with the permission of GlaxoSmithKline.
Background References
  1. Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
    Good et al.
    J.Med.Chem., 2013;56:1878
  2. Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism.
    Talapatra et al.
    J.Med.Chem., 2013;56:6317
  3. A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer.
    Jackson et al.
    First AACR International Conference on Molecular and Diagnostics in Cancer Therapeutic Development., 2006;:Abstract (B11)

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