LY3295668

Catalog No.S8782 Batch:S878201

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Technical Data

Formula

C24H26ClF2N5O2
Molecular Weight 489.95 CAS No. 1919888-06-4
Solubility (25°C)* In vitro DMSO 98 mg/mL (200.02 mM)
Ethanol 15 mg/mL (30.61 mM)
Water 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.)

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Biological Activity

Description LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
Targets
AURKA [1]
(Cell-free assay)
0.8 nM(Ki)
In vitro

LY3295668, an AURKA inhibitor with over 1,000-fold selectivity versus AURKB, is distinguished by minimal toxicity to bone marrow cells at concentrations active against RB1mut cancer cells.[1]
In vivo

LY3295668 leads to durable regression of RB1mut tumor xenografts at exposures that are well tolerated in rodents. Genetic suppression screens identifi ed enforcers of the spindle-assembly checkpoint (SAC) as essential for LY3295668 cytotoxicity in RB1-defi cient cancers and suggest a model in which a primed SAC creates a unique dependency on AURKA for mitotic exit and survival.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    NCI-H446 cells, Calu-6 cells

  • Concentrations

    0.001 μM - 1 μM

  • Incubation Time

    24 h, 48 h, 72 h

  • Method

    To measure apoptosis by IncuCyte Zoom instrument, NCI-H446 and Calu-6 cells are plated on Costar 3596 plates and treated with LY3295668 at different concentrations for 24, 48, and 72 hours. Caspase 3/7 activation is measured with Cell- Player 96-Well Kinetic Caspase 3/7 reagent. Green fluorescent images are acquired every 2 hours. Green objects counted (y-axis) are plotted against either real time (x-axis) or raw numbers as percent control.
Animal Study:

[1]
  • Animal Models

    7–8 week-old athymic nude female mice

  • Dosages

    50 mg/kg

  • Administration

    Oral gavage

Selleck's LY3295668 has been cited by 3 publications

Combination drug screen targeting glioblastoma core vulnerabilities reveals pharmacological synergisms [ EBioMedicine, 2023, 95:104752] PubMed: 37572644
BCL-xL inhibition potentiates cancer therapies by redirecting the outcome of p53 activation from senescence to apoptosis [ Cell Rep, 2022, 41(12):111826] PubMed: 36543138
Treatment of RB-deficient retinoblastoma with Aurora-A kinase inhibitor [ Kaohsiung J Med Sci, 2021, 10.1002/kjm2.12469] PubMed: 34741392

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.