Home Cell Cycle Aurora Kinase inhibitor TAK-901

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TAK-901 Aurora Kinase inhibitor

Cat.No.S2718

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 Aurora Kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 504.64

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Chemical Information, Storage & Stability

Molecular Weight 504.64 Formula

C28H32N4O3S

 Storage (From the date of receipt)
CAS No. 934541-31-8 Download SDF Storage of Stock Solutions

Synonyms N/A 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

Solubility

In vitro
Batch:

DMSO : 101 mg/mL (200.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
JAK3 [2]
1.2 nM
c-Src [2]
1.3 nM
CLK2 [2]
<2.0 nM
FGR [2]
<2.0 nM
YES1 [2]
<2.0 nM
LRRK2 [2]
3.0 nM
FLT3 [2]
5.0 nM
Fyn [2]
5.3 nM
ARG [2]
5.6 nM
Axl [2]
5.8 nM
Hck [2]
5.8 nM
SNF1LK2 [2]
6.0 nM
Abl [2]
6.4 nM
RET [2]
6.5 nM
TrkA [2]
6.7 nM
LCK [2]
6.8 nM
PTK5 [2]
7.1 nM
Fms [2]
7.2 nM
FGFR2 [2]
7.3 nM
EphB1 [2]
8.9 nM
Abl (T315I) [2]
9.0 nM
EphA1 [2]
9.1 nM
ARK5 [2]
9.1 nM
ITK [2]
12 nM
ALK2 [2]
13 nM
CDK7 [2]
14 nM
BLK [2]
14 nM
Aurora B-INCENP [1]
15 nM
JAK2 [2]
17 nM
EphB2 [2]
18 nM
Aurora A-TPX2 [1]
21 nM
STK16 [2]
24 nM
EphA2 [2]
24 nM
BRK [2]
25 nM
EphB4 [2]
27 nM
TNK2 [2]
27 nM
FGFR1 [2]
28 nM
EphA4 [2]
31 nM
STK33 [2]
35 nM
CLK1 [2]
45 nM
AMPK [2]
46 nM
FES [2]
48 nM
SLK [2]
49 nM
Chk2 [2]
50 nM
TYK2 [2]
54 nM
BTK [2]
55 nM
FAK2 [2]
55 nM
c-Kit [2]
58 nM
VEGFR2 [2]
60 nM
FGFR3 [2]
65 nM
ALK5 [2]
78 nM
MAP3K9 [2]
80 nM
CLK3 [2]
88 nM
JAK1 [2]
93 nM
In vitro
TAK-901 inhibits Aurora A-TPX2 and Aurora B-INCENP in tight binding, time-dependent manner. Dissociation of this compound from Aurora B-INCENP is slow with at 1/2 of 920 minutes, and the affinity constant for its binding to Aurora B-INCENP is determined to be 0.02 nM. It 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, this chemical 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 this agent with IC50 values similar to those for Aurora A and B. In cells, it 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, it inhibits the NFkB and JAK/STAT pathways with submicromolar potency. [1]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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