LY3295668

LY3295668 (AK-01) is a highly specific and orally active inhibitor of Aurora-A kinase with a Ki values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 avoids the formation of polyploids related to AurB inhibition. LY3295668 can be used for the study of small cell lung cancer[1][2].

Product Specifications

CAS Number

[1919888-06-4]

Product Name Alternative

AK-01

UNSPSC

12352005

Target

Apoptosis; Aurora Kinase

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LY3295668.html

Purity

99.76

Solubility

DMSO : 80 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C([C@@]1(CC2=NC(NC3=NNC(C)=C3)=CC=C2F)C[C@@H](C)N(CC4=CC=CC(Cl)=C4F)CC1)O

Molecular Formula

C24H26ClF2N5O2

Molecular Weight

489.95

References & Citations

[1]Gong X, et al. Aurora-A kinase inhibition is synthetic lethal with loss of the RB1 tumor suppressor gene. Cancer Discov. 2018 Oct 29. pii: CD-18-0469.|[2]Du J, et al. Aurora A-Selective Inhibitor LY3295668 Leads to Dominant Mitotic Arrest, Apoptosis in Cancer Cells, and Shows Potent Preclinical Antitumor Efficacy. Mol Cancer Ther. 2019 Dec;18 (12) :2207-2219.