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Aurora A/MYCN Dual Inhibitor, CD532-Calbiochem

品牌
Sigma-Aldrich
货号
5.32605
规格纯度
A cell permeable, highly potent, selective inhibitor of Aurora A (IC50 = 48 nM). Disrupts MYCN-Aurora A complex.
参考价格
2442.83 *本价格含增值税费
促销
服务
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数量
-+
产品名称:
Aurora A/MYCN Dual Inhibitor, CD532-Calbiochem
Aurora A Inhibitor, CD532, MYCN Inhibitor, CD532
产品介绍:

产品说明

一般描述

A cell permeable diaminopyrimidine derived compound that acts as a highly potent and selective inhibitor of Aurora A (IC50 = 48 nM). Acts by binding to the hinge region via a pyrazole moiety and stabilizes a DFG-in, inactive conformation of Aurora A. Potentiates the loss of the wild-type MYCN protein by disrupting MYCN-Aurora A complex and allowing its ubiquitination and proteasomal degradation in MYCN-amplified SK-N-BE (2) and Kelly neuroblastoma cells (EC50 = 223 and 146.7 nM, respectively). Causes a loss of S-phase entry of cells and allows their accumulation in both G0/G1 and G2 phases. Shown to be effective in vivo with serum t1/2 = 1.5 h in mice.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell permeable diaminopyrimidine derived compound that acts as a highly potent and selective inhibitor of Aurora A (IC50 = 48 nM). Acts by binding to the hinge region via a pyrazole moiety and stabilizes a DFG-in, inactive conformation of Aurora A. Potentiates the loss of the wild-type MYCN protein by disrupting MYCN-Aurora A complex and allowing its ubiquitination and proteasomal degradation in MYCN-amplified SK-N-BE (2) and Kelly neuroblastoma cells (EC50 = 223 and 146.7 nM, respectively). Causes a loss of S-phase entry of cells and allows their accumulation in both G0/G1 and G2 phases. Shown to be effective in vivo with serum t1/2 = 1.5 h in mice.

生化/生理作用

Cell permeable: yes
Primary Target
Aurora A
Secondary Target
MYCN
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Lee, J.K., et al. 2016. Cancer Cell.29, In press.
Gustafson, W. C., et al. 2014. Cancer Cell.26, 414.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C26H25F3N8O
分子量522.52
MDL编号MFCD32671941

产品性质

质量水平100
测定≥97% (HPLC)
形式solid
效能48 nM IC50
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 tan
溶解性DMSO: 50 mg/mL
储存温度2-8℃
SMILES stringO=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(NC3=NC=CC(NC4=NNC(C5CCCC5)=C4)=N3)C=C2

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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