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GSK923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E). GSK923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. GSK923295 demonstrated significant antitumor activity against solid tumor models, inducing CRs in Ewing sarcoma, rhabdoid, and rhabdomyosarcoma xenografts. GSK923295 exhibits robust, dose-dependent antitumor activity against Colo205 xenografts, including partial and complete regressions at the 125 mg/kg dose.
| Molecular Weight | 592.13 |
| Formula | C32H38ClN5O4 |
| CAS Number | 1088965-37-0 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Kinesin Products |
|---|
| Ispinesib
Ispinesib (SB 715992) is the first potent, highly specific small-molecule inhibitor of kinesin spindle protein (KSP) with an IC50 of 4.1 nM. |
| SB-743921
SB-743921 is a highly potent and active KSP inhibitor with a Ki of 0.1 nM for KSP (Eg5). |
| AZ3146
AZ3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor with IC50 of 35 nM. |
| MPI-0479605
MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases. |
| ARRY-520
ARRY-520 is a potent and selective kinesin spindle protein (KSP) inhibitor with an IC50 of 15 nM for A2780, CP70 and 01-28 cell lines in vitro. |
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