PF-573228 | FAK Inhibitor II | FAK Inhibitor | AmBeed-信号通路专用抑制剂

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PF-573228 99%+

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。

PF-573228 化学结构
CAS号：869288-64-2

PF-573228 3D分子结构
CAS号：869288-64-2

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PF-573228 纯度/质量文件产品仅供科研

货号：A230913 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024. Ambeed. [ A288696 ]; • JMC, 2024. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

FAK 亚型比较

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	99%+
PF-573228	+ FAK, IC50: 4 nM		99%+
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。

PF-573228 生物活性

靶点	FAK FAK, IC50:4 nM
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]

PF-573228 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
endothelial cell	40 nM	Function assay		inhibits H2O2-induced stress fiber formation	21212402

PF-573228 动物研究

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.

PF-573228 参考文献

[1]Slack-Davis JK, Martin KH, et al. Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007;282(20):14845-52.

[2]Zhao XK, Cheng Y, et al. Focal Adhesion Kinase Regulates Fibroblast Migration via Integrin beta-1 and Plays a Central Role in Fibrosis. Sci Rep. 2016.

PF-573228 实验方案

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

PF-573228 技术信息

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

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

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

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
endothelial cell	40 nM	Function assay	inhibits H2O2-induced stress fiber formation	21212402
endothelial cell	40 nM	Apoptosis assay	inhibits apoptosis	21212402
FasR	~10 μM	Kinase assay	inhibits the phosphorylation of FAK Tyr397 with IC50 of 130 nM	20354780
FasR	1 μM	Function assay	inhibits cell migration	20354780
F-G	~10 μM	Kinase assay	inhibits the phosphorylation of FAK Tyr397 with IC50 of 30 nM	17395594
GH3	3 μM	Function assay	increases IK(Ca) amplitude	21925512
GH3	3 μM	Function assay	enhances BKCa-channel activity	21925512
human peripheral blood T cells	~10 μM	Kinase assay	inhibits site-specific phosphorylation of FAK	23928188
human peripheral blood T cells	~10 μM	Function assay	impairs TCR-induced T cell morphological changes and alters activity of RhoA	23928188
human peripheral blood T cells	~10 μM	Function assay	inhibits phosphorylation of ZAP-70 and LAT	23928188
human peripheral blood T cells	~10 μM	Function assay	impairs Antigen-dependent T cell conjugation	23928188
HUVEC	~10 μM	cytotoxicity assay	impairs endothelial cell viability	22075057
HUVEC	5 μM	Kinase assay	inhibits FAK kinase activity	22075057
HUVEC	5 μM	Function assay	induces cell cycle arrest	22075057
HUVEC	5 μM	Apoptosis assay	induces apoptosis	22075057
HUVEC	5 μM	Function assay	impedes endothelial cell migration and alters the cellular actin cytoskeleton	22075057
HUVEC	5 μM	Function assay	blocks HUVEC sprouting on collagen I gels	22075057
L3.6p1	~10 μM	Kinase assay	inhibits the phosphorylation of FAK Tyr397 with IC50 of 300 nM	17395594
MCF7	~10 μM	Kinase assay	inhibits the phosphorylation of FAK Tyr397 with IC50 of 430 nM	20354780
MDCK	~10 μM	Kinase assay	inhibits the phosphorylation of FAK Tyr397 with IC50 of 500 nM	17395594
MDCK	10 μM	Apoptosis assay	induces apoptosis	17395594
PC3	~10 μM	Kinase assay	inhibits the phosphorylation of FAK Tyr397 with IC50 of 100 nM	17395594
PC3	10 μM	Growth inhibitory assay	significantly inhibits cell growth.	17395594
platelet	1 μM	Function assay	inhibits platelet aggregation and spreading	19716803
platelet	1 μM	Function assay	leads to inhibition of PAK and AKT	19716803
platelet	1 μM	Function assay	blocks calcium mobilization and dense granule secretion	19716803
REF52	~10 μM	Kinase assay	inhibits the phosphorylation of FAK Tyr397 with IC50 of ~100 nM	17395594
REF52	10 μM	Growth inhibitory assay	significantly inhibits cell growth.	17395594
REF52	10 μM	Apoptosis assay	induces apoptosis	17395594
REF52	10 μM	Function assay	blocks serum and FN-stimulated migration	17395594
SKOV-3	~10 μM	Kinase assay	inhibits the phosphorylation of FAK Tyr397 with IC50 of 50 nM	17395594
TamR	~10 μM	Kinase assay	inhibits the phosphorylation of FAK Tyr397 with IC50 of 50 nM	20354780
TamR	1 μM	Function assay	inhibits cell migration	20354780

PF-573228 99%+

PF-573228 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

PF-573228 质控信息

PF-573228 生物活性

PF-573228 细胞研究

PF-573228 动物研究

PF-573228 参考文献

PF-573228 实验方案

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PF-573228 99%+

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全球学术期刊中引用的产品

PF-573228 质控信息

PF-573228 生物活性

PF-573228 细胞研究

PF-573228 动物研究

PF-573228 参考文献

PF-573228 实验方案

PF-573228 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

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临床研究

确认信息

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PF-573228 纯度/质量文件产品仅供科研