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TAK-901

In stock
Catalog No.
A4124
Novel Aurora A/B inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$120.00
In stock
5mg
$110.00
In stock
10mg
$190.00
In stock
50mg
$590.00
In stock
200mg
$1,490.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 0.0017, 0.021 for Aurora-B/INCENP and Aurora-A/TPX2, respectively

Protein kinases Aurora A, B, and C play crucial roles during mitosis and cell division, are frequently elevated in cancer, and represent attractive targets for therapeutic intervention. TAK-901 is a novel, multitargeted Aurora B kinase inhibitor derived from a novel azacarboline kinase hinge-binder chemotype.

In vitro: TAK-901 exhibited time-dependent, tight-binding inhibition of Aurora B, but not Aurora A. Consistently, TAK-901 suppressed cellular histone H3 phosphorylation and induced polyploidy. In various human cancer cell lines, TAK-901 inhibited cell proliferation with effective concentration values from 40 to 500 nmol/L. TAK-901 potently inhibited only a few kinases other than Aurora B in intact cells, including FLT3 and FGFR2 [1].

In vivo: In rodent xenografts, TAK-901 exhibited potent activity against multiple human solid tumor types, and complete regression was found in the ovarian cancer A2780 model. In vivo biomarker studies showed that TAK-901 induced PD responses consistent with Aurora B inhibition and correlating with retention of TAK-901 in tumor tissue. [2].

Clinical trials: An open-label, dose escalation, phase I study has been conducted to identify the MTD and PK profile of TAK-901 in adult patients with advanced solid tumors or lymphoma.

Reference:
[1] Farrell P, Shi L, Matuszkiewicz J, Balakrishna D, Hoshino T, Zhang L, Elliott S, Fabrey R, Lee B, Halkowycz P, Sang B, Ishino S, Nomura T, Teratani M, Ohta Y, Grimshaw C, Paraselli B, Satou T, de Jong R.   Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor. Mol Cancer Ther. 2013;12(4):460-70.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt504.64
Cas No.934541-31-8
FormulaC28H32N4O3S
Solubility≥25.25 mg/mL in DMSO, <2.06 mg/mL in EtOH, <1.68 mg/mL in H2O
Chemical Name5-(3-ethylsulfonylphenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide
SDFDownload SDF
Canonical SMILESCCS(=O)(=O)C1=CC=CC(=C1)C2=CC(=C(C3=C2C4=CC(=CN=C4N3)C)C)C(=O)NC5CCN(CC5)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description TAK-901 is a novel inhibitor of Aurora A and B with IC50 value of 21 nM and 15 nM, respectively.
Targets Aurora A Aurora B        
IC50 21 nM 15 nM        

Quality Control

Quality Control & MSDS

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Chemical structure

TAK-901