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