产品
编 号：F741210
分子式：C19H23N9O2
分子量：409.45
分子式：C19H23N9O2
分子量：409.45
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 1432515-73-5
产品详情
生物活性：
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 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.
体内研究：
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 Cmax (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).Animal Model:Female BALB/c nude mice, with KBM5-T315I cells xenografted
Dosage:12.5?mg/kg, 25?mg/kg
Administration:Intraperitoneal injection, every 2 days, for 14 days
Result:Significantly inhibited the growth of tumors.
Animal Model:SD rats (220-280 g)
Dosage:2.5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:Intravenous injection, oral administration
Result:Oral bioavailability (28.7%), Cmax (202.4 μg/L), T1/2 (8.9 h)
体外研究：
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).
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 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.
体内研究：
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 Cmax (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).Animal Model:Female BALB/c nude mice, with KBM5-T315I cells xenografted
Dosage:12.5?mg/kg, 25?mg/kg
Administration:Intraperitoneal injection, every 2 days, for 14 days
Result:Significantly inhibited the growth of tumors.
Animal Model:SD rats (220-280 g)
Dosage:2.5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:Intravenous injection, oral administration
Result:Oral bioavailability (28.7%), Cmax (202.4 μg/L), T1/2 (8.9 h)
体外研究：
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).
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