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AKI603

CAS No. : 1432515-73-5

MCE 站：AKI603

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：Aurora Kinase

In Vitro: 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=21.01), Sk-br-3 (IC₅₀=0.73), MDA-MB-231 (IC₅₀=3.49), MDA-MB-453 (MTT, IC₅₀=0.18; Cell counting, IC₅₀=0.19), MDA-MB-468 (MTT, IC₅₀=0.15; Cell counting, IC₅₀=0.17).

In Vivo: 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).

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Epigenetics Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Cytoskeleton Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  AT9283  |  KW-2449  |  PF-03814735  |  ZM-447439  |  SNS-314 mesylate  |  CCT 137690  |  SCH-1473759 hydrochloride  |  NU6140  |  Aurora kinase inhibitor-2  |  Tripolin A  |  Aurora B inhibitor 1  |  Aurora inhibitor 1

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