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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. ARRY-520 had low nanomolar antiproliferative activity in tumor cell lines. ARRY-520 effectively reduced cell viability in a time-dependent manner in the Type II EOC cell lines A2780, CP70, and 01–28 but had minimal effect on Paclitaxel-resistant Type I EOC cell lines R182, 01–19b, and R1140. In addition, following ARRY-520 treatment, a significant increase in the activity of caspases- 8, 9, and 3 was observed in a time-dependent manner.ARRY-520 is able to induce the activation of caspase-2 in a time-dependent manner similar to that observed with the other caspases-9, -8, and -3. ARRY-520 is able to down-regulate the constitutive MCP-1 secretion. In addition, ARRY-520 induced a decrease in tumor kinetics in a dose-dependent manner.
| Molecular Weight | 420.48 |
| Formula | C20H22F2N4O2S |
| CAS Number | 885060-09-3 |
| 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. |
| 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. |
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