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    TCS7010 (Aurora A Inhibitor I)
    TCS7010 (Aurora A Inhibitor I)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0358
    CAS #: 1158838-45-9Purity ≥98%

    Description: TCS 7010 (Aurora A Inhibitor I; TCS-7010 ) is a novel, potent, and highly selective inhibitor of Aurora A kinase-AAK with potential antitumor activity. It inhibits Aurora A kinase with an IC50 of 3.4 nM in a cell-free assay and shows 1000-fold higher selectivity for Aurora A over Aurora B. TCS7010 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. 

    References: J Med Chem. 2009 May 28;52(10):3300-7; Carcinogenesis. 2012 Feb;33(2):285-93.

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    Molecular Weight (MW)588.07
    FormulaC31H31ClFN7O2
    CAS No.1158838-45-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 118 mg/mL (200.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: N-(2-Chlorophenyl)-4-[[2-[[4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]phenyl]amino]-5-fluoro-4-pyrimidinyl]amino]-benzamide

    InChi Key: AKSIZPIFQAYJGF-UHFFFAOYSA-N

    InChi Code: InChI=1S/C31H31ClFN7O2/c1-2-39-15-17-40(18-16-39)28(41)19-21-7-11-24(12-8-21)36-31-34-20-26(33)29(38-31)35-23-13-9-22(10-14-23)30(42)37-27-6-4-3-5-25(27)32/h3-14,20H,2,15-19H2,1H3,(H,37,42)(H2,34,35,36,38)

    SMILES Code: O=C(NC1=CC=CC=C1Cl)C2=CC=C(NC3=NC(NC4=CC=C(CC(N5CCN(CC)CC5)=O)C=C4)=NC=C3F)C=C2

    SynonymsTC S 7010; TCS 7010; TC-S7010



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    In Vitro

    In vitro activity: Aurora A Inhibitor I is a 2,4-dianilinopyrimidine that selectively and potently inhibits Aurora A. Aurora A Inhibitor I effectively inhibits the proliferation of HCT116 and HT29 cells, with IC50 of 190 nM and 2.9 μM, respectively. The Aurora A selectivity of Aurora A Inhibitor I against Aurora B depends on a single amino acid (Thr217) of Aurora A. In KCL-22 cells, Aurora A Inhibitor I (1-5 μM) increases G2/M cell fraction, induces histone H3 serine 10 phosphorylation, and suppresses mitotic Aurora A autophosphorylation on Thr288. Aurora A Inhibitor I (0.5-5 μM) also suppresses cell proliferation in KCL-22 cells, as well as BCR-ABL-negative leukemia cell lines KG-1 and HL-60. Aurora A Inhibitor I effectively induces apoptosis in KCL-22 cells at 5 μM. In a recent study, Aurora A Inhibitor I is also found to inhibit cell growth of HCT116, HT29, and HeLa cells, with IC50 of 377.6 nM, 5.6 μM, and 416 nM.


    Kinase Assay: Both Auroras A and B are assayed in ELISA format using a GST fusion (pGEX-4T) of the N-terminus of Histone H3 (aa 1−18) as substrate. Plates are coated with 2 μg/mL substrate in PBS then blocked with 1 mg/mL I-block in PBS. Kinase reactions are run for 40 min with 5 ng/mL (0.16 nM) Aurora A or 45 ng/mL (1.1 nM) Aurora B at 30 μM ATP (~ Km) in kinase buffer. Final DMSO concentration is 4%. Product is detected by incubation with antiphosphohistone H3 (Ser10) 6G3 mouse monoclonal antibody and sheep-anti-mouse HRP conjugate, followed by washing and addition of TMB substrate. After quenching with 1 M phosphoric acid, plates are read at 450 nM.


    Cell Assay: Cells (HCT116 and HT29 cells) are seeded in 384-well plates on day 0 in 50 μL of complete medium and incubated overnight in a 5% CO2atmosphere at 37 °C. On day 1, 10 μL of Aurora A Inhibitor I is added. On day 4, plates are allowed to reach room temperature, and 30 μL Cell Titer-Glo reagent is added to each well to measure total ATP levels. Plates are read after shaking 15 min at room temperature.

    In VivoNA
    Animal modelNA
    Formulation & DosageNA
    References

    J Med Chem. 2009 May 28;52(10):3300-7; Carcinogenesis. 2012 Feb;33(2):285-93; ACS Chem Biol. 2012 Jan 20;7(1):185-96.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Aurora A Inhibitor I

    Aurora A Inhibitor I (Compound 1) Inhibits Intracellular Functions of Aurora A and B. ACS Chem Biol. 2012 Jan 20; 7(1): 185–196.


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