LY3295668

Catalog No.S8782 Batch:S878201

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 RB1^mut cancer cells.^[1]

In vivo

LY3295668 leads to durable regression of RB1^mut 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

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

References

[1] Xueqian Gong, et al. Cancer Discov. 2019 Feb;9(2):248-263.

Selleck's LY3295668 has been cited by 6 publications

RET overexpression leads to increased brain metastatic competency in luminal breast cancer [ J Natl Cancer Inst, 2024, djae091]	PubMed: 38852945
Combination of an aurora kinase inhibitor and the ABL tyrosine kinase inhibitor asciminib against ABL inhibitor-resistant CML cells [ Med Oncol, 2024, 41(6):142]	PubMed: 38714583
Combination drug screen targeting glioblastoma core vulnerabilities reveals pharmacological synergisms [ EBioMedicine, 2023, 95:104752]	PubMed: 37572644
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.

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