LY-3295668 (AK-01)

Background Information:

LY3295668 (LY-3295668, AK-01) is an orally available, potent and
highly selective Aurora A kinase (AurA) inhibitor with Ki of 0.8 nM, and
H446 AurA auto-P IC₅₀ of 0.6 nM, highly selective (>1000 fold) over Aurora B. LY3295668 is cytotoxic to RB1 mutant cancer cells (NCI-H446 cell IC₅₀ = 0.752 uM), and achieves durable regression of RB1mut tumor xenografts.

Reference:

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.

APIM050193: LY-3295668 (AK-01)

CAS No.: 1919888-06-4.
Molecular Formula: C₂₄H₂₆ClF₂N₅O₂ • 0.2H₂O.
Molecular Weight: 493.6.
Purity: >99% by achiral and chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, 1H-NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.