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.
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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.
Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism.
Talapatra et al.
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)