Home Cell Cycle Aurora Kinase inhibitor TAK-901 For research use only.

TAK-901

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.

TAK-901 Chemical Structure

TAK-901 Chemical Structure

CAS No. 934541-31-8

Purity & Quality Control

TAK-901 Related Products

Signaling Pathway

Aurora Kinase Signaling Pathways

Aurora Kinase Signaling Pathway

Biological Activity

Description 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.
Targets
JAK3 [2] c-Src [2] CLK2 [2] FGR [2] YES1 [2] Click to View More Targets
1.2 nM 1.3 nM <2.0 nM <2.0 nM <2.0 nM
In vitro
In vitro 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. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00935844 Completed
Advanced Solid Tumors|Lymphoma
Millennium Pharmaceuticals Inc.
 October 2009 Phase 1
NCT00807677 Completed
Acute Myeloid Leukemia|Acute Lymphoblastic Leukemia|Chronic Myelogenous Leukemia|Chronic Lymphocytic Leukemia|Multiple Myeloma|Waldenstrom''s Macroglobulinemia|Myelodysplastic Syndrome|Philadelphia Chromosome-negative CML|Myeloid Metaplasia|Myelofibrosis|Advanced Polycythemia|Non-Hodgkins Lymphoma
Millennium Pharmaceuticals Inc.
 March 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 504.64 Formula

C28H32N4O3S
CAS No. 934541-31-8 SDF Download TAK-901 SDF
Smiles CCS(=O)(=O)C1=CC=CC(=C1)C2=CC(=C(C3=C2C4=C(N3)N=CC(=C4)C)C)C(=O)NC5CCN(CC5)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 101 mg/mL ( (200.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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