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/ Aurora Kinase / AKI603

AKI603 {[allProObj[0].p_purity_real_show]}

货号：A1483447 Ambeed 开学季，买赠积分，赢豪礼

AKI603是一种针对 AurA 的抑制剂，展示了克服白血病中的耐药性突变和抗增殖活性的潜力。

AKI603 化学结构 CAS号：1432515-73-5
AKI603 化学结构
CAS号：1432515-73-5
AKI603 3D分子结构
CAS号：1432515-73-5
AKI603 化学结构 CAS号：1432515-73-5
AKI603 3D分子结构 CAS号：1432515-73-5
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AKI603 纯度/质量文件 产品仅供科研

货号：A1483447 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Aurora A ↓ Aurora B ↓ Aurora C ↓ 其他靶点 纯度
BI-847325 ++

Aurora A (Human), IC50: 25 nM

 		++++

Aurora B (Xenopus laevis), IC50: 3 nM

 		++

Aurora C (Human), IC50: 15 nM

 		{[allProObj[0].p_purity_real_show]}
CCT 137690 ++

Aurora A, IC50: 15 nM

 		++

Aurora B, IC50: 25 nM

 		++

Aurora C, IC50: 19 nM

 		{[allProObj[0].p_purity_real_show]}
MK-5108 ++++

Aurora A, IC50: 0.064 nM

 		{[allProObj[0].p_purity_real_show]}
KW-2449 +

Aurora A, IC50: 48 nM

 		FLT3 {[allProObj[0].p_purity_real_show]}
Tozasertib ++++

Aurora A, Ki app: 0.6 nM

 		++

Aurora B, Ki app: 18 nM

 		+++

Aurora C, Ki app: 4.6 nM

 		FLT3,Bcr-Abl {[allProObj[0].p_purity_real_show]}
AT9283 ++++

Aurora A, IC50: ~3.0 nM

 		++++

Aurora B, IC50: ~3.0 nM

 		{[allProObj[0].p_purity_real_show]}
MLN8054 +++

Aurora A, IC50: 4 nM

 		+

Aurora B, IC50: 172 nM

 		{[allProObj[0].p_purity_real_show]}
ZM-447439 +

Aurora A, IC50: 110 nM

 		+

Aurora B, IC50: 130 nM

 		Src {[allProObj[0].p_purity_real_show]}
TCS7010 ++++

Aurora A, IC50: 3.4 nM

 		{[allProObj[0].p_purity_real_show]}
TAK-901 ++

Aurora A-TPX2, IC50: 21 nM

 		++

Aurora B-INCENP, IC50: 15 nM

 		{[allProObj[0].p_purity_real_show]}
Danusertib +++

Aurora A, IC50: 13 nM

 		+

Aurora B, IC50: 79 nM

 		+

Aurora C, IC50: 61 nM

 		RET {[allProObj[0].p_purity_real_show]}
MK-8745 ++++

Aurora A, IC50: 0.6 nM

 		{[allProObj[0].p_purity_real_show]}
PHA-680632 ++

Aurora A, IC50: 27 nM

 		+

Aurora B, IC50: 135 nM

 		+

Aurora C, IC50: 120 nM

 		FLT3 {[allProObj[0].p_purity_real_show]}
AMG 900 +++

Aurora A, IC50: 5 nM

 		+++

Aurora B, IC50: 4 nM

 		++++

Aurora C, IC50: 1 nM

 		{[allProObj[0].p_purity_real_show]}
Alisertib ++++

Aurora A, IC50: 1.2 nM

 		{[allProObj[0].p_purity_real_show]}
ENMD-2076 +++

Aurora A, IC50: 14 nM

 		+

Aurora B, IC50: 350 nM

 		FLT3,RET {[allProObj[0].p_purity_real_show]}
JNJ-7706621 +++

Aurora A, IC50: 11 nM

 		++

Aurora B, IC50: 15 nM

 		{[allProObj[0].p_purity_real_show]}
CYC-116 +++

Aurora A, Ki: 8 nM

 		+++

Aurora B, Ki: 9 nM

 		FLT3 {[allProObj[0].p_purity_real_show]}
Reversine +++

Aurora A, IC50: 12 nM

 		+++

Aurora B, IC50: 13 nM

 		++

Aurora C, IC50: 20 nM

 		{[allProObj[0].p_purity_real_show]}
CCT129202 ++

Aurora A, IC50: 42 nM

 		+

Aurora B, IC50: 198 nM

 		+

Aurora C, IC50: 227 nM

 		{[allProObj[0].p_purity_real_show]}
SNS-314 mesylate +++

Aurora A, IC50: 9 nM

 		++

Aurora B, IC50: 31 nM

 		++++

Aurora C, IC50: 3 nM

 		{[allProObj[0].p_purity_real_show]}
Barasertib-HQPA ++++

Aurora B, IC50: 0.37 nM

 		{[allProObj[0].p_purity_real_show]}
Hesperadin +

Aurora B (human), IC50: 250 nM

 		{[allProObj[0].p_purity_real_show]}
GSK-1070916 ++++

Aurora B-INCENP, IC50: 3.5 nM

 		+++

Aurora C-INCENP, IC50: 6.5 nM

 		SIK,Tie-2 {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

AKI603 生物活性

描述 AKI603, an Aurora kinase A (AurA) inhibitor with an IC50 of 12.3 nM, is designed to counteract resistance from the BCR-ABL-T315I mutation. It demonstrates potent anti-proliferative effects in leukemic cells[1][2].
体内研究

AKI603 (12.5-25 mg/kg; i.p.; every 2 days; for 14 days) eliminates the growth of KBM5-T315I xenografts in nude mice[1].

Following oral administration in rats (25 mg/kg), AKI603 demonstrates moderate oral bioavailability (28.7%) and a peak concentration (Cmax) of 202.4 μg/L[3].

After intravenous administration in rats (2.5 mg/kg), AKI603 has a terminal elimination half-life of 8.9 hours[3].
体外研究

AKI603 (0.039-0.6 μM; 48 hours) greatly suppresses the growth of leukemia cells[1].

AKI603 (0.039-0.6 μM; 48 hours) markedly reduces AurA phosphorylation in NB4, K562, and Jurkat cells in a dose-dependent way without altering total AurA protein levels[1].

AKI603 hampers both the growth and colony-forming ability of imatinib-resistant CML cells[1].

AKI603 (0.3-0.6 μM; 48 hours) reduces cell growth and the ability to form colonies in imatinib-resistant CML cells by triggering cell cycle arrest and polyploidy accumulation[1].

Inhibition of AURA by AKI603 induces the bleaching of the BCR-ABL cell regulator in wild-type and T315I mutant cells [1].

AKI603 shows effectiveness in inhibiting the proliferation of breast cancer cells, with IC50 values as follows: SUM149 (2.04), BT549 (0.86), MCF-7 (0.97), MCF-7-Epi (21.01), Sk-br-3 (0.73), MDA-MB-231 (3.49), MDA-MB-453 (MTT, 0.18; Cell counting, 0.19), MDA-MB-468 (MTT, 0.15; Cell counting, 0.17)[2].

AKI603 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.

AKI603 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.42mL

4.88mL

2.44mL

AKI603 技术信息

CAS号1432515-73-5
分子式C19H23N9O2
分子量 409.44
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 120 mg/mL(293.08 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: AKI603 | 1432515-73-5 | AKI 603 | AKI-603 | AurA Inhibitor | Cell Cycle/DNA Damage | Epigenetics | Aurora Kinase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | AKI603 纯度/质量文件 | AKI603 亚型比较 | AKI603 生物活性 | AKI603 参考文献 | AKI603 实验方案 | AKI603 技术信息

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