LY3295668

Synonyms: AK-01

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.

LY3295668 Chemical Structure

LY3295668 Chemical Structure

CAS: 1919888-06-4

Selleck's LY3295668 has been cited by 3 publications

Purity & Quality Control

Batch: S878201 DMSO] 98 mg/mL] false] Ethanol] 15 mg/mL] false] Water] Insoluble] false Purity: 99.49%
99.49

LY3295668 Related Products

Choose Selective Aurora Kinase Inhibitors

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
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]

Cell Research 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.

In Vivo
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]

Animal Research Animal Models 7–8 week-old athymic nude female mice
Dosages 50 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03898791 Completed
Small Cell Lung Cancer
Eli Lilly and Company
July 16 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 489.95 Formula

C24H26ClF2N5O2

CAS No. 1919888-06-4 SDF --
Smiles CC1CC(CCN1CC2=C(C(=CC=C2)Cl)F)(CC3=C(C=CC(=N3)NC4=NNC(=C4)C)F)C(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 98 mg/mL ( (200.02 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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