AKI603 是一种极光激酶 A (AurA) 抑制剂，其 IC₅₀ 值为 12.3 nM，被开发用于克服白血病中 BCR-ABL-T315I 耐药性突变。AKI603 对白血病细胞具有很强的抗增殖活性。

AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC 50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.

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Aurora A 12.3 nM (IC50)

AKI603 (0.039-0.6 μM; 48 hours) extensively inhibits proliferation of leukemia cells.
AKI603 (0.039-0.6 μM; 48 hours) 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.
AKI603 inhibits the proliferation and colony formation of imatinib resistant CML cells.
AKI603 (0.3-0.6 μM; 48 hours) inhibits cell proliferation and colony formation capacities in imatinib-resistant CML cells by inducing cell cycle arrest with polyploidy accumulation.
Inhibition of AurA by AKI603 induces leukemia cell senescence in both BCR-ABL wild type and T315I mutation cells.
AKI603 exhibits inhibitory activities on breast cancer cell proliferation, such as SUM149 (IC50=2.04), BT549 (IC50=0.86), MCF-7 (IC50=0.97), MCF-7-Epi (IC50

AKI603 (12.5-25?mg/kg; i.p.; every 2 days; for 14 days) abrogates the growth of xenografted KBM5-T315I cells in nude mice.
AKI603 exhibits moderate oral bioavailability (rat 28.7%) and C max (rat 202.4 μg/L) following oral administration (rat 25 mg/kg).
AKI603 exhibits terminal elimination half-life (rat 8.9 h) following intravenous administration (rat 2.5 mg/kg).
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Le-Xun Wang, et al. Aurora A Kinase Inhibitor AKI603 Induces Cellular Senescence in Chronic Myeloid Leukemia Cells Harboring T315I Mutation. Sci Rep. 2016 Nov 8;6:35533.
[2]. Fei-Meng Zheng, et al. A novel small molecule aurora kinase inhibitor attenuates breast tumor-initiating cells and overcomes drug resistance. Mol Cancer Ther. 2014 Aug;13(8):1991-2003.

In Vitro: DMSO : 125 mg/mL (305.29 mM; Need ultrasonic)配制储备液