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CAS No.: 879127-16-9

Aurora kinase inhibitor-3 Catalog No. CSN23770

Synonyms: Aurora Kinase Inhibitor III;AKI-7169

Aurora kinase inhibitor III is a potent ATP-competitive aurora related kinase (also designated ARK) inhibitor with IC50 value of 42 nM for Aurora A kinase.

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技术信息

生物活性

描述The Aurora family of serine/threonine kinases are essential for mitotic progression. Mammals express three paralogs; Aurora A, Aurora B, and Aurora C. The three enzymes share highly similar catalytic domains, but show different subcellular localization. Potent inhibitors of Aurora A and B kinases, have been shown to be so effective at suppressing tumor growth in vivo that they have progressed into clinical trials. Aurora Kinase Inhibitor III is an Aurora A kinase (AIKA) with IC₅₀ of 42 nM, and only weakly inhibit EGFR with IC₅₀ > 10 μM. The inhibitor binding mode is novel, with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket, and several induced structural changes in the active-site compared with other published AIK structures^[1].
作用机制Aurora Kinase Inhibitor III adopts a s-cis conformation upon binding to AIK, exposing most of the available hydrogen-bonding groups on the inhibitor to the interior of the active-site. The dipyrimidine and aniline moieties bind in a classical adenine mimetic fashion, forming two hydrogen bonds with main chain atoms from A213 in the hinge region^[1].
参考文献

[1] Tari LW, Hoffman ID, Bensen DC, Hunter MJ, Nix J, Nelson KJ, McRee DE, Swanson RV. Structural basis for the inhibition of Aurora A kinase by a novel class of high affinity disubstituted pyrimidine inhibitors. Bioorg Med Chem Lett. 2007 Feb 1;17(3):688-91.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4190 mL
- 12.0949 mL
- 24.1899 mL
- 5 mM
- 0.4838 mL
- 2.4190 mL
- 4.8380 mL
- 10 mM
- 0.2419 mL
- 1.2095 mL
- 2.4190 mL

技术信息

CAS号

879127-16-9

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H18F3N5O

运输

蓝冰

分子量

413.40

别名

Aurora Kinase Inhibitor III;AKI-7169

溶解度

DMSO	115.0 mg/mL (278.2 mM)
Water	insoluble

动物实验配方

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