Molecular Formula | C31H34Cl2N2O3 |
Molar Mass | 553.51926 |
Solubility | H2O: soluble5mg/mL, clear |
Appearance | powder |
Color | white to beige |
Storage Condition | -20°C |
In vitro study | SB 743921 has K I values of 0.1 nM and 0.12 nM for human and murine KSP, respectively, and K I values of greater than 70 μm for the other Kinks MKLP1 and kin2. 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 study | SB-743921 can effectively inhibit P388 leukemia 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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.807 ml | 9.033 ml | 18.066 ml |
5 mM | 0.361 ml | 1.807 ml | 3.613 ml |
10 mM | 0.181 ml | 0.903 ml | 1.807 ml |
5 mM | 0.036 ml | 0.181 ml | 0.361 ml |
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. |