Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AKI603 是一种极光激酶 A 抑制剂,IC50值为 12.3 nM。它对白血病细胞具有很强的抗增殖活性,可用于克服白血病中 BCR-ABL-T315I 耐药性突变。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
5 mg | ¥ 2,890 | 现货 | ||
10 mg | ¥ 4,330 | 现货 | ||
25 mg | ¥ 6,920 | 现货 | ||
50 mg | ¥ 9,360 | 现货 | ||
100 mg | ¥ 12,600 | 现货 | ||
500 mg | ¥ 25,200 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,110 | 现货 |
产品描述 | 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]. |
靶点活性 | Aurora A:12.3 nM |
体外活性 | 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]. |
体内活性 | 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]. |
细胞实验 | 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]. 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]. |
动物实验 | AKI603 (12.5-25?mg/kg; i.p.; every 2 days; for 14 days; female BALB/c nude mice with KBM5-T315I cells xenografted) abrogates the growth of tumors[1]. Pharmacokinetic Analysis shows that AKI603 exhibits moderate oral bioavailability (rat 28.7%) and Cmax (rat 202.4 μg/L) following oral administration (rat 25 mg/kg)[3]. AKI603 also exhibits terminal elimination half-life (rat 8.9 h) following intravenous administration (rat 2.5 mg/kg)[3]. |
别名 | AKI 603, AKI-603 |
分子量 | 409.45 |
分子式 | C19H23N9O2 |
CAS No. | 1432515-73-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (293.07 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4423 mL | 12.2115 mL | 24.423 mL | 61.0575 mL |
5 mM | 0.4885 mL | 2.4423 mL | 4.8846 mL | 12.2115 mL | |
10 mM | 0.2442 mL | 1.2212 mL | 2.4423 mL | 6.1058 mL | |
20 mM | 0.1221 mL | 0.6106 mL | 1.2212 mL | 3.0529 mL | |
50 mM | 0.0488 mL | 0.2442 mL | 0.4885 mL | 1.2212 mL | |
100 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6106 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AKI603 1432515-73-5 Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase chronic CML leukemia myeloid inhibit imatinib-resistant Inhibitor AKI 603 AKI-603 inhibitor