A potent Eg5 inhibitor (IC50 = 6 nM); selective for Eg5 over a panel of 8 kinesins (IC50s = >100 μM) and a panel of 224 kinases at 10 μM; induces time-and dose-dependent cell death in HL-60

ARRY-520 – 25 mg

Brand:
Cayman
CAS:
885060-09-3
Storage:
-20
UN-No:
Non-Hazardous - /

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 μM) and a panel of 224 kinases at a concentration of 10 μM. 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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Description

A potent Eg5 inhibitor (IC50 = 6 nM); selective for Eg5 over a panel of 8 kinesins (IC50s = >100 μM) and a panel of 224 kinases at 10 μM; induces time-and dose-dependent cell death in HL-60, Jurkat, OCI-AML3, U937, and MOLM-13 leukemic cells; induces cell cycle arrest at the G2/M phase in a p53- and XIAP-independent manner in OCI-AML3 cells; inhibits blast colony formation of bone marrow samples derived from human AML patients; completely eliminates tumors in the RPMI-8226 multiple myeloma and HL-60 and MV4-11 AML mouse xenograft models at 20 mg/kg per day ,

Formal name: (2S)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3(2H)-carboxamide

Synonyms:  Filanesib

Molecular weight: 420.5

CAS: 885060-09-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53

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