半岛bd体育手机客户端 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 effectivein vivowith 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 effectivein vivowith 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 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | solid |
| 效能 | 48 nM IC50 |
| manufacturer/tradename | Calbiochem? |
| 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 string | O=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 |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
