biological activity | SB743921 is a kinesin spindle protein (KSP) inhibitor, ki is 0.1 nM and has little affinity for MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. Phase 1/2. |
Target | TargetValue KSP (MX1 cells) 0.06 nM KSP (Colo205 cells) 0.07 nM KSP 0.1 nM(Ki) KSP (SKOV3 cells) 0.2 nM KSP (MV522 cells) 1.7 nM |
Target | Value |
KSP (MX1 cells)
| 0.06 nM |
KSP (Colo205 cells)
| 0.07 nM |
KSP
| 0.1 nM(Ki) |
KSP (SKOV3 cells)
| 0.2 nM |
KSP (MV522 cells)
| 1.7 nM |
in vitro study | The K I values of SB 743921 for human and mouse KSP are 0.1 nM and 0.12 nM, respectively, for the other kinesin MKLP1 and Kin2, the K I values were greater than 70 μm. SB 743921 blocks the assembly of a functional mitotic spindle, thus blocking cells during mitosis and subsequently leading to cell necrosis. SB-743921 potency against ispinesib has been improved in biochemical and cellular experiments, respectively. |
in vivo studies | is effective in inhibiting P388 leukemia SB-743921 in vivo. Unlike taxanes, SB-743921 had a significant effect on a broad-spectrum tumor model. SB-743921 pairs of xenografted human tumors Colo205 (complete regression), MCF-7, SK-MES, H69, OVCAR-3 (complete and partial regression) and HT-29, MX-1, MDA-MB-231, A2780 (tumor growth delay) can produce growth-inhibiting activity. SB-743921 does not cause neuropathies frequently associated with tubulin. |