324878
Focal Adhesion Kinase Inhibitor II
The Focal Adhesion Kinase Inhibitor II, also referenced under CAS 869288-64-2, controls the biological activity of Focal Adhesion Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
Focal Adhesion Kinase Inhibitor II, PF-573,228, PF-228, 6-((4-((3-(Methanesulfonyl)benzyl)amino)-5-trifluoromethylpyrimidin-2-yl)amino)-3,4-dihydro-1H-quinolin-2-one, FAK Inhibitor II, Cdk7 Inhibitor V
质量水平
方案
≥97% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
off-white
溶解性
DMSO: 50 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C22H20F3N5O3S/c1-34(32,33)16-4-2-3-13(9-16)11-26-20-17(22(23,24)25)12-27-21(30-20)28-15-6-7-18-14(10-15)5-8-19(31)29-18/h2-4,6-7,9-10,12H,5,8,11H2,1H3,(H,29,31)(H2,26,27,28,30)
InChI key
HESLKTSGTIBHJU-UHFFFAOYSA-N
一般描述
A cell-permeable pyrimidinyldiamino compound that acts as a selective, ATP-competitive, and potent FAK inhibitor (IC50 = 4 nM). It inhibits CDK7/cycH/MAT1 and CDK1/cycB only at much higher concentrations (IC50 = 197 and 486 nM, respectively) and exhibits little or much reduced activity against 39 other commonly studied kinases (≤64% inhibition at 1 µM). PF-573,228 effectively inhibits cellular FAK Tyr397 phosphorylation in various human, rat, and canine cell lines (IC50 = ~30-500 nM during an 1 h incubation period) and concomitant blockage of Tyr31 phosphorylation of the FAK downstream substrate paxillin is also demonstrated in rat fibroblast REF52 cultures. A useful tool for studying FAK-mediated cellular functions.
其他说明
Slack-Davis, J.K., et al. 2007. J. Biol. Chem.282, 14845.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
No data available
闪点(°C)
No data available
Chien-Chung Huang et al.
Cells, 10(8) (2021-08-28)
Angiogenesis is a critical process in the formation of new capillaries and a key participant in rheumatoid arthritis (RA) pathogenesis. Vascular endothelial growth factor (VEGF) stimulation of endothelial progenitor cells (EPCs) facilitates angiogenesis and the progression of RA. Phosphorylation of
Lohit Khera et al.
Life science alliance, 4(6) (2021-04-01)
Cancer stem cells (CSCs) are implicated in tumor initiation, metastasis and drug resistance, and considered as attractive targets for cancer therapy. Here we identified a clinically relevant signaling nexus mediated by AXL receptor, PYK2 and PKCα and show its impact
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