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
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
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
off-white
solubility
DMSO: 50 mg/mL
shipped in
ambient
Quality Level
General description
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.
Other Notes
Slack-Davis, J.K., et al. 2007. J. Biol. Chem.282, 14845.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
No data available
flash_point_c
No data available
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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