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.

• Synonyma: 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
• Empirický vzorec (Hillův zápis): C₂₂H₂₀F₃N₅O₃S
• Číslo CAS: 869288-64-2
• Molekulová hmotnost: 491.49
• UNSPSC Code: 12352200
• MDL number: MFCD11519967
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze

Vlastnosti

• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: off-white
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 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

Popis

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)

Bezpečnostní informace

• pictograms: GHS07
• signalword: Warning
• hcodes: H302
• pcodes: P264 - P270 - P301 + P312 - P501
• Hazard Classifications: Acute Tox. 4 Oral
• Skladovací třída: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: No data available
• flash_point_c: No data available