产品说明
一般描述
A cell-permeable phenylcarbamoylfuran-carboxamide compound that acts as a potent, selective, and reversible inhibitor of poly(ADP-ribosyl)ation activity of tankyrase 1 and 2 (IC50 = 1.9 and 0.83 µM, respectively). Exhibits high selectivity over PARP1 (IC50 = 20 µM). Stabilizes and increases AXIN2 levels, thereby enhancing phosphorylation and degradation of β-catenin resulting in reduced canonical Wnt signaling (IC50 = 470 nM in Wnt 3a-induced HEK293 cells transfected with ST-Luc). Shown to induce cell cycle arrest and diminish the proliferation of SW480 colorectal cancer cells (~ 5 µM). Suppresses tumor growth in tamoxifen-induced polyposis in Apc knock-out murine model (100 mg/kg, i.p.). Displays adequate human liver microsomal stability (t1/2 = 10.1 min).
包装
25 mg in Glass bottle
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
tankyrase 1 and 2
Reversible: yes
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Waaler, J., et al. 2012. Cancer Res.72, 2822.
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 | C25H26N2O5 |
| 分子量 | 434.48 |
| MDL编号 | MFCD03863265 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥99% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | off-white |
| 溶解性 | DMSO: 100 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
| SMILES string | O=C(NCC1(CCOCC1)C2=CC=C(C=C2)OC)C3=CC=C(NC(C4=CC=CO4)=O)C=C3 |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
