Aurora Kinase Inhibitor 3

Aurora Kinase Inhibitor 3用途

Aurora Kinase Inhibitor 3 是一种有效的,选择性 Aurora A 激酶抑制剂,IC50 为 42 nM,同时微弱抑制 EGFR,IC50>10 μM。Aurora Kinase Inhibitor 3 的环丙烷羧酸部分指向 ATP 结合口袋的溶剂暴露区域,并且与其他公开的 AIK 结构相比,活性位点中存在几种诱导的结构变化。

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Aurora Kinase Inhibitor 3名称

[ CAS 号 ]:
879127-16-9

[ 中文名 ]:
极光激酶抑制剂III

[ 英文名 ]:
Aurora Kinase Inhibitor 3

[英文别名 ]:

Anilinopyrimidine1
2np8
Aurora Kinase Inhibitor III

Aurora Kinase Inhibitor 3生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> 极光激酶

信号通路 >> 细胞周期/DNA损伤 >> 极光激酶

研究领域 >> 其他

[ 靶点 ]

Aurora A:42 nM (IC50)

[参考文献]

[1]. Tari LW, et al. Structural basis for the inhibition of Aurora A kinase by a novel class of high affinitydisubstituted pyrimidine inhibitors. Bioorg Med Chem Lett. 2007 Feb 1;17(3):688-91.

Aurora Kinase Inhibitor 3物理化学性质

[ 分子式 ]:
C₂₁H₁₈F₃N₅O

[ 分子量 ]:
413.39600

[ 精确质量 ]:
413.14600

[ PSA ]:
85.66000

[ LogP ]:
5.47550

[ 储存条件 ]:
-20°C，密闭，干燥

Aurora Kinase Inhibitor 3安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933599090

Aurora Kinase Inhibitor 3海关

[ 海关编码 ]: 2933599090

[ 中文概述 ]:
2933599090. 其他结构上有嘧啶环的化合物(包括其他结构上有哌嗪环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Aurora Kinase Inhibitor 3文献

Synthetic lethal screen of an EGFR-centered network to improve targeted therapies.

Sci. Signal. 3 , ra67, (2010)

Intrinsic and acquired cellular resistance factors limit the efficacy of most targeted cancer therapeutics. Synthetic lethal screens in lower eukaryotes suggest that networks of genes closely linked t...

Enhanced genetic instability and dasatinib sensitivity in mammary tumor cells lacking NEDD9.

Cancer Res. 70 , 8907-16, (2010)

Elevated expression of the NEDD9/HEF1/Cas-L scaffolding protein promotes tumor cell invasion and metastasis in multiple cancer cell types. Conversely, generation of mammary tumors in the mouse mammary...

Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library.

J. Am. Chem. Soc. 128 , 2182-2183, (2006)

The epidermal growth factor receptor (EGFR) tyrosine kinase was one of the first receptor tyrosine kinases to be targeted for drug development by the pharmaceutical industry due to its ubiquitous over...

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