Focal Adhesion Kinase Inhibitor I-CAS 4506-66-5-Calbiochem

C₆H₁₀N₄ · 4HCl

284.01

MFCD00012970

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).
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 autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC₅₀<1 M) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 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 M) and in mice in vivo (~25% of no treatment controls on day 23; 30 mg/kg via 5 i.p/wk).

Toxicity: Standard Handling (A)

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

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

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

100

≥95% (elemental analysis)

solid

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

gray

water: 14 mg/mL
DMSO: 50 mg/mL

ambient

2-8℃

1S/C6H10N4.4ClH/c7-3-1-4(8)6(10)2-5(3)9;;;;/h1-2H,7-10H2;4*1H

BZDGCIJWPWHAOF-UHFFFAOYSA-N

Packaged under inert gas

11 - Combustible Solids

WGK 3