ARRY-520

ARRY-520

CAT N°: 21883
Price:

48.00 40.80

ARRY-520 is a potent inhibitor of the kinesin spindle protein Eg5 (IC50 = 6 nM).{42111} It is selective for Eg5 over a panel of 8 kinesins (IC50s = >100 ?M) and a panel of 224 kinases at a concentration of 10 ?M. ARRY-520 induces time-and dose-dependent cell death in HL-60, Jurkat, OCI-AML3, U937, and MOLM-13 leukemic cells.{42112} Downregulation of Eg5 expression sensitizes HL-60 cells to ARRY-520 (IC50s = 11.3 and 2 nM for wild-type and Eg5 knockdown HL-60 cells, respectively). ARRY-520 induces cell cycle arrest at the G2/M phase in a p53- and XIAP-independent manner in OCI-AML3 cells. It also inhibits blast colony formation of bone marrow samples derived from human acute myeloid leukemia (AML) patients. In vivo, ARRY-520 (20 mg/kg per day) completely eliminates tumors in the RPMI-8226 multiple myeloma and HL-60 and MV4-11 AML mouse xenograft models.{42111}

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