Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

General description

A cell-permeable quinazoline compound that acts as a potent and reversible CXCR4 antagonist (IC₅₀ = 36.2 nM for SDF-1/CXCL12 binding to hCXCR4-transfected HEK293 membrane) with selectivity over closely related human chemokine receptors CXCR2, CCR2, CCR4 and CCR5 (IC₅₀ >10 µM). Shown to inhibit CXCL12-induced Ca²⁺-mobilization and cell migration in hCXCR4-HEK293 cells (IC₅₀ = 100.1 and 41 nM, respectively), and rapidly mobilize CXCR4⁺, CD34⁺ and CD133⁺ stem cells from bone marrow in C57BL/6 male mice (6 mg/kg, s.c).

Legal Information

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

Other Notes

Wu, C.H., et al. 2012. Chem. Med. Chem.7, In press.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)