PF-573228CAS号： 869288-64-2分子式： C22H20F3N5O3S分子量： 491.49描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM. |
| 纯度 |
98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 别名 |
PF 573228
|
| 外观 |
white to off-white powder
|
| 可溶性/溶解性 |
DMSO : 49.2 mg/mL (100 mM)
|
| 生物活性 | |
| 靶点 |
FAK
|
| In vitro(体外研究) |
PF 573228 blocks the phosphorylation of FAK Tyr397 in REF52 cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of 30-500 nM. However, PF 573228 (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with PF-228 resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover.
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| In vivo(体内研究) |
Inhibition of FAK by PF-573,228 in Ctrl-MT mice leads to a significant suppression of mammary tumorigenesis as well as lung metastasis. In contrast, treatment of MFCKO-MT mice with PF-573,228 did not affect the initiation of mammary tumors in these mice, as would be expected due to the JPence of FAK in mammary epithelial cells of these mice .
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| 参考文献 | |
| 参考文献 |
[1] Slack-Davis JK, et al. J Biol Chem, 2007, 282(20), 14845-14852. |
分子结构图
