AKI603

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

AKI603  纯度: 98.05%

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

AKI603 Chemical Structure

CAS No. : 1432515-73-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg ¥58000 In-stock
25 mg ¥110000 In-stock
50 mg ¥170000 In-stock
100 mg ¥250000 In-stock
200 mg   询价  
500 mg   询价  

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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[1][2].

IC50 & Target[1]

Aurora A

12.3 nM (IC50)

体外研究
(In Vitro)

AKI603 (0.039-0.6 μM; 48 hours) extensively inhibits proliferation of leukemia cells[1].
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[1].
AKI603 inhibits the proliferation and colony formation of imatinib resistant CML cells[1].
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[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, 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)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: U937 cells, HL-60 cells, NB4 cells, KBM5 cells, K562 cells, Jurkat cells
Concentration: 0.039 μM, 0.078 μM, 0.16 μM, 0.3 μM, 0.6 μM
Incubation Time: 48 hours
Result: Inhibited all the tested cell lines.

Western Blot Analysis[1]

Cell Line: NB4 cells, K562 cells, Jurkat cells
Concentration: 0.039 μM, 0.078 μM, 0.16 μM, 0.3 μM, 0.6 μM
Incubation Time: 48 hours
Result: Inhibited the phosphorylation of AurA Thr288 (p-AurA).

Cell Cycle Analysis[1]

Cell Line: K562, K562/G, 32D-p210 and 32D-T315I cells
Concentration: 0.3 μM, 0.6 μM
Incubation Time: 48 hours
Result: Induced polyploidization in the tested cells.

体内研究
(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[1].
AKI603 exhibits moderate oral bioavailability (rat 28.7%) and Cmax (rat 202.4 μg/L) following oral administration (rat 25 mg/kg)[3].
AKI603 exhibits terminal elimination half-life (rat 8.9 h) following intravenous administration (rat 2.5 mg/kg)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice, with KBM5-T315I cells xenografted[1]
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)[3]
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)

分子量

409.45

Formula

C19H23N9O2

CAS 号

1432515-73-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (305.29 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4423 mL 12.2115 mL 24.4230 mL
5 mM 0.4885 mL 2.4423 mL 4.8846 mL
10 mM 0.2442 mL 1.2212 mL 2.4423 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 6.25 mg/mL (15.26 mM); Suspended solution; Need ultrasonic

    此方案可获得 6.25 mg/mL (15.26 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [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.

    [3]. Zhenzhen Zhao, et al. Determination of a novel Aurora-A (AurA) kinase AKI603 by UPLC-MS/MS and its application to a bioavailability study in rat. J Pharm Biomed Anal. 2016 Jun 5;125:303-9.

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