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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.
APIM050042: LY3295668 (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.
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