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FAK inhibitor 5

Chemical Structure : FAK inhibitor 5

CAS No.: 2237234-47-6

FAK inhibitor 5

Catalog No.: PC-35210Not For Human Use, Lab Use Only.

FAK inhibitor 5 is the first highly potent, selective irreversible inhibitor of the FAK kinase with IC50 of 0.6 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

FAK inhibitor 5 is the first highly potent, selective irreversible inhibitor of the FAK kinase with IC50 of 0.6 nM; displays little to no inhibition against a panel of ten kinases (EGFR, HER2/ERBB2, IGF1R, c-Kit, PDGFR, Pyk2, c-Src, IRR, and IR); dose-dependently inhibits the proliferation with ED50 of 1.73 uM in SCC cells, blocks Tyr397 phosphorylation in a dose-dependent manner and significantly inhibits FAK autophosphorylation at low concentrations.

Physicochemical Properties

M.Wt 575.026
Formula C28H27ClN8O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((2-((4-(((2-((2-acrylamidoethyl)amino)-3,4-dioxocyclobut-1-en-1-yl)amino)methyl)phenyl)amino)-5-chloropyrimidin-4-yl)amino)-N-methylbenzamide

References

1. Yen-Pon E, et al. ACS Chem Biol. 2018 Jun 13. doi: 10.1021/acschembio.8b00250.

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