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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Related Kinesin Products|
Monastrol is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles.
AZD4877 is a synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity.
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.
GSK923295 is an allosteric inhibitor of CENP-E with Ki value of 3.2 nM.
AZ3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor with IC50 of 35 nM.
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