Name: TAK-901
Price: 292.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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.
    
    [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.
- Properties
  - Alternative Name
    
    5-(3-ethylsulfonylphenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide
    
    CAS Number
    
    934541-31-8
    
    Molecular Formula
    
    C28H32N4O3S
    
    Molecular Weight
    
    504.64
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥25.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

TAK-901

TAK-901

Background

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