324877

Focal Adhesion Kinase Inhibitor I

The Focal Adhesion Kinase Inhibitor I, also referenced under CAS 4506-66-5, controls the biological activity of Foca Adhesion Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : Focal Adhesion Kinase Inhibitor I, FAK Inhibitor I, 1,2,4,5-Benzenetetraamine, 4HCl, NSC 667249
• Formule empirique (notation de Hill) : C₆H₁₀N₄ · 4HCl
• Numéro CAS: 4506-66-5
• Poids moléculaire : 284.01
• UNSPSC Code: 12352200
• NACRES: NA.54
• MDL number: MFCD00012970
• Assay: ≥95% (elemental analysis)
• Form: solid
• Storage condition: OK to freeze, desiccated (hygroscopic), protect from light

Propriétés

• Quality Segment: 100
• assay: ≥95% (elemental analysis)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, desiccated (hygroscopic), protect from light
• color: gray
• solubility: water: 14 mg/mL, DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: Cl.Cl.Cl.Cl.Nc1c(cc(c(c1)N)N)N
• InChI: 1S/C6H10N4.4ClH/c7-3-1-4(8)6(10)2-5(3)9;;;;/h1-2H,7-10H2;4*1H
• InChI key: BZDGCIJWPWHAOF-UHFFFAOYSA-N

Description

General description

A cell-permeable tetraamine compound that is identified from a computer-aided molecular docking screening based on Fak Y397 interaction and is shown to inhibit FAK (Cat. No. 324876) autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC₅₀<1 µM) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 (Cat. No. 662067) autophosphorylation or the kinase activity of c-Raf, c-Src, EGFR, VEGFR-3, IGF-1, Met, PDGFR-α, Pyk2, and PI 3-K (p110δ/p85α). Reported to inhibit BT474 proliferation both in cultures in vitro (IC₅₀ ~10 µM) and in mice in vivo (~25% of no treatment controls on day 23; 30 mg/kg via 5 i.p/wk).

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Golubovskaya, V.M., et al. 2008. J. Med. Chem.51, 7405.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Informations sur la sécurité

• Classe de stockage: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable