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LY3295668 Aurora Kinase inhibitor

Cat.No.S8782

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 Aurora Kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 489.95

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 98 mg/mL (200.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

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

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Chemical Information, Storage & Stability

Molecular Weight 489.95 Formula

C24H26ClF2N5O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1919888-06-4 -- Storage of Stock Solutions

Synonyms AK-01 Smiles CC1CC(CCN1CC2=C(C(=CC=C2)Cl)F)(CC3=C(C=CC(=N3)NC4=NNC(=C4)C)F)C(=O)O

Mechanism of Action

Targets/IC50/Ki
AURKA
(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.
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 this compound 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03898791 Completed
Small Cell Lung Cancer
Eli Lilly and Company
 July 16 2019 Phase 1

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