A cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition in kinase assays and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1uM with 30 min inhibitor preincubation), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38alpha, Pyk2, or Src even at concentrations as high as 10uM.
Synonyms:FAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide
Molecular Formula:C₂₂H₂₆N₄O₂S
Solubility:DMSO
Primary Target:FAK
Purity:≥99% (HPLC)
Appearance:Off-white powder.
Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.