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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.

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C22H20F3N5O3S
CAS Number:
869288-64-2
Molecular Weight:
491.49
MDL number:
MFCD11519967
UNSPSC Code:
12352200

Quality Level

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

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.

Warning

Toxicity: Standard Handling (A)

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

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

No data available

flash_point_c

No data available

Certificates of Analysis (COA)

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