LY3295668 (AK-01)

LY3295668 is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively.

Signaling Pathways >> Cell Cycle/DNA Damage >> Aurora Kinase

Signaling Pathways >> Epigenetics >> Aurora Kinase

Research Areas >> Cancer

Aurora A:0.8 nM (IC50)

LY3295668 is a highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively. LY3295668, a highly specific AurA inhibitor, can kill Rb-deficient cancer cells at doses that have minimal effects on normal cells. In a kinome-wide survey, only 5 of 386 kinases are potently inhibited by LY3295668 (<10 nM)[1].

[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.

Alisertib (MLN8237) | Tozasertib | AT9283 | Barasertib (AZD1152-HQPA) | danusertib | Hesperadin | Reversine | MLN8054 | GSK1070916 | AMG-900 | KW-2449 | TAK-632 | TAK-901 | MK-5108(VX-689) | pf-03814735