5.04045

Focal Adhesion Kinase Inhibitor III

• Sinônimo(s): Focal Adhesion Kinase Inhibitor III, N-(4- tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide, FAK Inhibitor III
• Fórmula empírica (Notação de Hill): C₂₂H₂₆N₄O₂S
• Número CAS: 1426683-53-5
• Peso molecular: 410.53
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥99% (HPLC)
• Nível de qualidade: 100
• forma: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: off-white
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

A cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition against FAK kinase activity in cell-free assays (IC₅₀ = 0.64 and 2.2 µM, respectively, with 60 or 5 min FAK-inhibitor preincubation before substrate poly-GT and 0.5 µM ATP addition) and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC₅₀ = 7.1 µM with 30 min inhibitor preincubation before 2 h stimulation by plating cells on fibronectin-coated surface), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38α, Pyk2, or Src even at concentrations as high as 10 µM.

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 = 7.1 µM with 30 min inhibitor preincubation), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38α, Pyk2, or Src even at concentrations as high as 10 µM.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
FAK

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Tomita, N., et al. 2013. Bioorg. Med. Chem. Lett.23, 1779.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable