货号:A230913 同义名: FAK Inhibitor II;Focal Adhesion Kinase Inhibitor II
PF-573228 是一种有效且选择性的 FAK 抑制剂,对纯化的重组 FAK 催化片段的 IC50 值为 4 nM。
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产品名称 | FAK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Defactinib | ✔ | 99%+ | |||||||||||||||||
NVP-TAE 226 |
++
PYK2, IC50: 3.5 nM FAK, IC50: 5.5 nM |
Insulin Receptor,IGF-1R | 98+% | ||||||||||||||||
PF-573228 |
+
FAK, IC50: 4 nM |
98% | |||||||||||||||||
Solanesol | ✔ | 90% +(HPLC) | |||||||||||||||||
PF-431396 |
++
PYK2, IC50: 11 nM FAK, IC50: 2 nM |
99%+ | |||||||||||||||||
PND-1186 |
++++
FAK, IC50: 1.5 nM |
99%+ | |||||||||||||||||
PF-562271 |
++++
PYK2, IC50: 13 nM FAK, IC50: 1.5 nM |
99%+ | |||||||||||||||||
GSK2256098 |
++++
FAK, Ki: 0.4 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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 | |
endothelial cell | 40 nM | Function assay | inhibits H2O2-induced stress fiber formation | 21212402 | |
Dose | Mice: 5 mg/kg[3] (p.o.), 125 mg/kg[4] (i.p.), 100 mg/kg[5] (i.v.) |
Administration | p.o., i.p., i.v. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.03mL 0.41mL 0.20mL |
10.17mL 2.03mL 1.02mL |
20.35mL 4.07mL 2.03mL |
CAS号 | 869288-64-2 |
分子式 | C22H20F3N5O3S |
分子量 | 491.486 |
别名 | FAK Inhibitor II;Focal Adhesion Kinase Inhibitor II |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
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 |
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 |