TCS7010 (Aurora A Inhibitor I)

Catalog No.S1451 Batch:S145104

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Technical Data

Formula

C31H31ClFN7O2
Molecular Weight 588.07 CAS No. 1158838-45-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (170.04 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description TCS7010 (Aurora A Inhibitor I) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway.
Targets
Aurora A [1]
(Cell-free assay)
3.4 nM
In vitro

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. [1] 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. [2] 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. [3]
Features Aurora A Inhibitor I is a novel, potent, and selective inhibitor to Aurora A.

Protocol (from reference)

Kinase Assay:

[1]
  • Auroras A and B Inhibition Assays

    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:

[1]
  • Cell lines

    HCT116 and HT29 cells

  • Concentrations

    0.1 nM - 10 μM, dissolved in medium lacking serum and glutamine (dissolved in DMSO as stock solution)

  • Incubation Time

    72 hours

  • Method

    Cells are seeded in 384-well plates on day 0 in 50 μL of complete medium and incubated overnight in a 5% CO2 atmosphere 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.
Animal Study:

[5]
  • Animal Models

    BALB/c nude mice bearing ARID1A isogenic tumors

  • Dosages

    30 and 60 mg/kg

  • Administration

    IP

Customer Product Validation

Data from [J Neurosci, 2012, 32, 11050-11066]

Data from [J Neurosci, 2012, 32, 11050-11066]

, , Dr. Zhang of Tianjin Medical University

Selleck's TCS7010 (Aurora A Inhibitor I) has been cited by 36 publications

Primary Cilia Restrain PI3K-AKT Signaling to Orchestrate Human Decidualization [ Int J Mol Sci, 2022, 23(24)15573] PubMed: 36555215
Primary Cilia Restrain PI3K-AKT Signaling to Orchestrate Human Decidualization [ Int J Mol Sci, 2022, 23(24)15573] PubMed: 36555215
Phospholipase D1 promotes astrocytic differentiation through the FAK/AURKA/STAT3 signaling pathway in hippocampal neural stem/progenitor cells [ Biochim Biophys Acta Mol Cell Res, 2022, 1869(12):119361] PubMed: 36162649
In vitro human cell-based aneugen molecular mechanism assay [ Environ Mol Mutagen, 2022, 63(3):151-161] PubMed: 35426156
Repression of the AURKA-CXCL5 axis induces autophagic cell death and promotes radiosensitivity in non-small-cell lung cancer [ Cancer Lett, 2021, 509:89-104] PubMed: 33848520
Aurora B-dependent polarization of the cortical actomyosin network during mitotic exit [ EMBO Rep, 2021, e52387] PubMed: 34431205
Exploiting loss of heterozygosity for allele-selective colorectal cancer chemotherapy. [ Nat Commun, 2020, 11(1):1308] PubMed: 32161261
MECP2 Mutations Affect Ciliogenesis: A Novel Perspective for Rett Syndrome and Related Disorders [ EMBO Mol Med, 2020, 8;e10270] PubMed: 32383329
ULK1-ATG13 and Their Mitotic Phospho-Regulation by CDK1 Connect Autophagy to Cell Cycle [ PLoS Biol, 2020, 9;18(6):e3000288] PubMed: 32516310
Cell division requires RNA eviction from condensing chromosomes [ J Cell Biol, 2020, 219(11)e201910148] PubMed: 33053167

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SHIPPING AND STORAGE
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