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SB-743921 is a kinesin spindle protein inhibitor with IC50 of 0.2 nM, 0.07 nM, 1.7 nM, 0.06 nM and 14.4 nM in SKOV3, Colo205, MV522, MX1 and P388 cell lines, respectively. SB-743921 selectively inhibits kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. SB 743921 blocks assembly of a functional mitotic spindle, thereby causing cell cycle arrest in mitosis and subsequent cell death. SB-743921 has significant efficacy in a broad spectrum of tumor models differing from that of taxanes. The maximum-tolerated dose (MTD) of SB-743921 as a 1-h infusion every 21 days was established as 4 mg/m(2). SB-743921 has entered in a Phase I clinical trial in the treatment of cancer.
| Molecular Weight | 553.52 |
| Formula | C31H33N2O3.HCl |
| CAS Number | 940929-33-9 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL Ethanol ≥ 60 mg/mL |
| 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. |
| AZ3146
AZ3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor with IC50 of 35 nM. |
| GSK923295
GSK923295 is an allosteric inhibitor of CENP-E with Ki value of 3.2 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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