AKI603 is a novel small molecule inhibitor of Aurora kinase A (AurA)(IC50 = 12.3 nM). AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells[1][2].

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

DMSO:120 mg/mL (293.07 mM)

Aurora A:12.3 nM

AKI603 inhibits the proliferation and colony formation of imatinib resistant CML cells[1]. Inhibition of AurA by AKI603 induces leukemia cell senescence in both BCR-ABL wild type and T315I mutation cells[1]. AKI603 exhibits inhibitory activities on breast cancer cell proliferation as well as significantly inhibits the phosphorylation of AurA in NB4, K562 and Jurkat cell lines in a dose-dependent manner while the level of total AurA protein is not changed[1].

AKI603 exhibits moderate oral bioavailability and Cmax following oral administration[3]. AKI603 exhibits terminal elimination half-life following intravenous administration[3]. AKI603 abrogates the growth of xenografted KBM5-T315I cells in nude mice[1].