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CAS No.: 869288-64-2

PF-573228 Catalog No. CSN16483

Synonyms: FAK Inhibitor II;Focal Adhesion Kinase Inhibitor II;PF-573,228

PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for inhibiton of purified recombinant catalytic fragment of FAK and inhibits FAK phosphorylation on Tyr(397) with an IC(50) of 30-100 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 FAK

IC50:4nM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Mice: 5 mg/kg^[3] (p.o.), 125 mg/kg^[4] (i.p.), 100 mg/kg^[5] (i.v.)

给药途径
p.o., i.p., i.v.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[3] (p.o.), 125 mg/kg^[4] (i.p.), 100 mg/kg^[5] (i.v.)
给药途径	p.o., i.p., i.v.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0346 mL
- 10.1732 mL
- 20.3465 mL
- 5 mM
- 0.4069 mL
- 2.0346 mL
- 4.0693 mL
- 10 mM
- 0.2035 mL
- 1.0173 mL
- 2.0346 mL

技术信息

CAS号

869288-64-2

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H20F3N5O3S

运输

蓝冰

分子量

491.49

别名

FAK Inhibitor II;Focal Adhesion Kinase Inhibitor II;PF-573,228

溶解度

DMSO	380.0 mg/mL (773.2 mM) warming
Water	insoluble

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

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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 Catalog No. CSN16483

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