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Aurora A/MYCN Dual Inhibitor, CD532-Calbiochem
| 产品编号： | 4083640 |
| 规格： | A cell permeable, highly potent, selective inhibitor of Aurora A (IC50 = 48 nM). Disrupts MYCN-Aurora A complex. |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
Aurora A/MYCN Dual Inhibitor, CD532-Calbiochem
Aurora A Inhibitor, CD532, MYCN Inhibitor, CD532
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C26H25F3N8O |
| Molecular weight | 522.52 |
| MDL number | MFCD32671941 |
| General description【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. |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Primary Target Aurora A Secondary Target MYCN Reversible: yes |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
| Other Notes【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. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥97% (HPLC) |
| form【形式】 | solid |
| potency【效能】 | 48 nM IC50 |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | tan |
| solubility【溶解性】 | DMSO: 50 mg/mL |
| storage temp.【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 |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
