产品说明书
PF-573228
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同义名 : | FAK Inhibitor II;Focal Adhesion Kinase Inhibitor II |
| CAS号 : | 869288-64-2 | |
| 货号 : | A230913 | |
| 分子式 : | C22H20F3N5O3S | |
| 纯度 : | 98% | |
| 分子量 : | 491.486 | |
| MDL号 : | MFCD11519967 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(50.87 mM)，配合低频超声助溶，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 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+30% PEG300+water 7 mg/mL clear PO 0.5% CMC-Na 27 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | FAK (Focal adhesion kinase), a non-receptor tyrosine kinase, can regulate cell migration, proliferation and survival through regulation on integrin and growth factor signaling pathways. PF-573228 is a selective FAK inhibitor with IC50 value of 4nM (measured by the purified recombinant catalytic fragment of FAK). Treatment with PF-573228 showed cellular FAK inhibition with IC50 of 11nM in A431 cells, and caused dose-dependent inhibition of p-FAK-Y397 with IC50 value of 100nM, 50nM, 300nM, 30nM and 500nM for PC3, SKOV-3, L3.6p1, F-G and MDCK cells. The decrease of paxillin, the downstream substrate of FAK, on its Tyr31 site was achieved by 1μM PF-573228 within 15min, showing the FAK signaling inhibition by PF-573228. Also a dose-dependent decrease by PF-573228 in FAK phosphorylation within paxillin-containing focal adhesions can be observed at concentration ranging in 0.3-3μM in REF52 cells. Pre-treatment with PF-573228 for 30min before 10% serum or fibronectin for 6h caused inhibition of serum- or fibronectin-stimulated migration of REF52 cells at concentration of 1μM with 80% p-FAK inhibition, but the random migration of REF52 cells was observed at concentration up to 10μM[1]. Inhibition of FAK by intraperitoneal injection of 50 mg/kg PF-573228 reduced signaling cascade of fibroblast migration in bleomycin-challenged mice[2]. | ||
| 作用机制 | PF-573228 is a competitive inhibitor of ATP with specificity for FAK family protein-tyrosine kinases.[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 |
| 4T1 | Function assay | abolishes the interaction between β3 integrin and TβR-II | 19740433 | ||
| A431 | ~10 μM | Kinase assay | inhibits FAK phosphorylation with IC50 of 11 nM | 17395594 | |
| endothelial cell | 40 nM | Kinase assay | inhibits H2O2-induced phosphorylation of FAK | 21212402 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.03mL 0.41mL 0.20mL |
10.17mL 2.03mL 1.02mL |
20.35mL 4.07mL 2.03mL |
| 参考文献 |
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