TAK-901 934541-31-8

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Molecular Weight:

504.64 TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a Potent Inhibitor of cellular JAK2, c-Src or Abl. Phase 1.


Biological Activity


TAK-901 inhibits Aurora A-TPX2 and Aurora B-INCENP in tight binding,
time-dependent manner. Dissociation of TAK-901 from Aurora B-INCENP is
slow with at 1/2 of 920 minutes, and the affinity constant for TAK-901
binding to Aurora B-INCENP is determined to be 0.02 nM. TAK-901 induces
inhibition of cell proliferation in cultured human cancer cell lines
from different tissues with IC50s ranging from 40 to 500nM.


Consistent
with Aurora B inhibition, TAK-901 treatment produces polyploidy in human
PC3 prostate cancer and HL60 acute myeloid leukemia cells as measured
by immunofluorescence and flow cytometry. Examination of a broad panel
of kinases reveals that multiple kinases, including FLT3, FGFR and the
Src family kinases, are inhibited by TAK-901 with IC50 values similar to
those for Aurora A and B.


In cells, TAK-901 suppresses the Flt3 and
FGFR2 autophosphorylation with IC50 values close to that of Aurora B as
measured by cellular histone H3 phosphorylation, whereas the IC50s for
inhibition of cellular Src and Bcr Abl are 20-fold weaker. In a panel of
pathway specific reporter-based cell models, TAK-901 inhibits the NFkB
and JAK/STAT pathways with submicromolar potency.

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Product Categories : Epigenetics > Aurora Kinase Inhibitor