TAK-901

Catalog No.S2718

TAK-901 Chemical Structure

Molecular Weight(MW): 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.

Size Price Stock Quantity  
In DMSO USD 340 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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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]
1.2 nM 1.3 nM <2.0 nM <2.0 nM <2.0 nM
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]

Protocol

Solubility (25°C)

In vitro DMSO 101 mg/mL (200.14 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
2% DMSO +30% PEG 300+2% Tween 80+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 504.64
Formula

C28H32N4O3S

CAS No. 934541-31-8
Storage powder
Synonyms N/A

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Clinical Trial Information

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|Waldenstroms Macroglobulinemia|Myelodysplastic Syndrome|Philadelphia Chromosome-negative CML|Myeloid Metaplasia|Myelofibrosis|Advanced Polycythemia|Non-Hodgkins Lymphoma Millennium Pharmaceuticals, Inc. March 2009 Phase 1

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

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

Aurora Kinase Signaling Pathway Map

Related Aurora Kinase Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID