产品说明书
PF-562271 besylate
 |
同义名 : | VS-6062 besylate;PF-562271 (besylate);PF-00562271 Besylate |
| CAS号 : | 939791-38-5 | |
| 货号 : | A554072 | |
| 分子式 : | C27H26F3N7O6S2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 665.664 | |
| MDL号 : | MFCD14105612 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 20 mg/mL(30.05 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
4% DMSO+30% PEG 300+water 3 mg/mL |
| 生物活性 | |||
|---|---|---|---|
| 描述 | FAK (Focal adhesion kinase), a non-receptor tyrosine kinase, can regulate the cytoskeleton and act as a scaffolding and signaling protein for other adhesion molecules. The expression of FAK and its phosphorylation status show a strong correlation with the invasive phenotype of aggressive human tumors. PF-562271 Besylate is the besylate form of PF-562271. PF-562271 is a potent and selective inhibitor for FAK and Pyk2 with IC50 values of 1.5nM and 14nM (measured by recombinant kinase assay), respectively, displaying over 100-fold selectivity against the other kinases tested[1]. PF-562271 showed robust inhibition on p-FAK with IC50 of 5nM in an inducible cell-based assay. Oral administration of PF-562271 can inhibit p-FAK in a dose-dependent fashion with calculated EC50 of 93ng/ml in the tumor-bearing mice, which suggesting the pharmacodynamics of this compound. In vitro study showed that PF-562271 had antitumor efficacy or caused tumor regression in multiple human s.c. xenograft models, including BxPC3, LoVo, U87MG, H125, PC3M and BT474, with dose ranging in 25-100mg/kg according to different models[1]. | ||
| 作用机制 | PF-562271 can bind in the ATP-binding cleft of FAK and form two of the three H-bonds between PF-562271 and main-chain atoms in the kinase hinge region.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| ALL-PO cell | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=1.01584 μM | SANGER | ||
| human 8305C cell | Growth inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50=1.09904 μM | SANGER | ||
| human AGS cell | Growth inhibition assay | Inhibition of human AGS cell growth in a cell viability assay, IC50=1.52124 μM | SANGER | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.50mL 0.30mL 0.15mL |
7.51mL 1.50mL 0.75mL |
15.02mL 3.00mL 1.50mL |
