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AKI603
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AKI603图片
CAS NO:1432515-73-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。
生物活性

AKI603 is an inhibitor ofAurora kinaseA (AurA), with anIC50of 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].

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].

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

性状

Solid

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.4423 mL12.2115 mL24.4230 mL
5 mM0.4885 mL2.4423 mL4.8846 mL
10 mM0.2442 mL1.2212 mL2.4423 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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本网站选购。