TAK-960

Athymic nude mice (BALB/cAJc1-nu/nu), severe combined immunodeficiency (SCID) mice (C.B17-Icr- scid/scid Jcl) or NOD-scid mice (NOD.CB17-Prkdc scid/J)

4-(9-cyclopentyl-7, 7-difluoro-5-methyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido[4, 5-b][1, 4]diazepin-2-ylamino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide

0.001-1uM

30 mg/kg

Suspended in 0.5% methyl cellulose

TAK-960 has shown activity in several tumor cell lines including those that express multidrug resistant protein 1 (MDR1). [1] Consistent with PLK1 inhibition, TAK-960 treatment gives rise to accumulation of G2/M cells, aberrant "polo" mitosis morphology, and increases phosphorylation of histone H3 (pHH3). [1] TAK-960 inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM, but not in non-dividing normal cells (EC50 >1, 000 nM). The mutation status of TP53 or KRAS and MDR1 expression does not correlate with the potency of TAK-960 in the cell lines tested. [1]

72 hours

Cells are seeded into 96-well plates at 3-30, 103 cells/well in appropriate medium plus 10% fetal calf serum (FCS). After 24 hours, cells are treated with serial dilutions of TAK-960, and 72 hours later, the number of viable cells is assessed using the CellTiter-Glo Assay. Calculation of EC50 values and statistical analysis are done.

TAK-960 Chemical Structure